EP2862562A1 - Cosmetic or dermatological composition for lightening and for preventing skin blemishes - Google Patents

Cosmetic or dermatological composition for lightening and for preventing skin blemishes Download PDF

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Publication number
EP2862562A1
EP2862562A1 EP20140157686 EP14157686A EP2862562A1 EP 2862562 A1 EP2862562 A1 EP 2862562A1 EP 20140157686 EP20140157686 EP 20140157686 EP 14157686 A EP14157686 A EP 14157686A EP 2862562 A1 EP2862562 A1 EP 2862562A1
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EP
European Patent Office
Prior art keywords
acid
dicarboxylic acid
skin
cosmetic
lightening
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Granted
Application number
EP20140157686
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German (de)
French (fr)
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EP2862562B1 (en
Inventor
Ira Hartmann
Marianne Waldmann-Laue
Soraya Heinen
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Henkel AG and Co KGaA
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Henkel AG and Co KGaA
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Publication of EP2862562A1 publication Critical patent/EP2862562A1/en
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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/362Polycarboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin

Definitions

  • the present invention relates to cosmetic or dermatological compositions for the cosmetic and topical dermatological skin whitening or for the prevention of tanning of the skin, in particular the skin tanning caused by UV radiation, and for the lightening of age spots or freckles.
  • the present invention further relates to the use of these agents and methods using these agents.
  • melanocytes which are found in the lowest layer of the epidermis in addition to the basal cells as either isolated or frequently occurring pigment-forming cells depending on the skin type.
  • Melanocytes contain melanosomes in which melanin is formed. Through various chemical and / or physical influences, in particular by UV radiation, melanin is increasingly formed. This is transported via the keratinocytes into the corneocytes (horny layer) and leads to a brownish to brown-black skin color.
  • Melanin is formed as the final stage of an oxidative process in which tyrosine is converted by means of the enzyme tyrosinase via several intermediates to the brown to brown-black eumelanins (DHICA and DHI melanin) or with the involvement of sulfur-containing compounds to the reddish phaeomelanin.
  • Melanin formation - and thus skin color - is subject to external influences and, in addition to desirable effects ("healthy tan”), can also lead to undesired symptoms.
  • benign tan may also occur due to genetic disposition, wound healing or scarring, or skin aging ("age spots"). Since the process of desquamation (superficial detachment of cells or cell groups from their epithelial dressing) involves a constant loss of melanin, lightening of the skin can be achieved by inhibiting the new synthesis of melanin.
  • Age spots are a sign of aging that requires special treatment. Age spots are not a more intensive pigmentation of the skin, but actually accumulations of the brownish-waxy pigment lipofuscin (also age or wear pigment), which is the end product of the oxidation of unsaturated fatty acids of cell membranes. The lysosomes are no longer able to completely degrade the substance. So he stays back as a stain.
  • Effective cosmetic skin whitening agents are known. However, these usually contain as active ingredient hydroquinone or kojic acid (for the inhibition of tyrosinase). Both substances are mutagenic and should therefore not be used for prolonged periods.
  • Skin cosmetic agents for the treatment of age spots are described, for example, in the European patent application EP 2163238 A2 described.
  • compositions according to the invention contain as the first obligatory component, based on the total weight of the compositions according to the invention, a total of from 0.001 to 2.0% by weight, preferably from 0.01 to 0.5% by weight and in particular from 0.05 to 0.2% by weight .-% of at least one extract from Quassia Amara.
  • the Quassia amara, Brazilian Quassia tree, Quassia tree, Quassia tree, Bitter quassia or as some other species also called Bitter wood is a plant species in the family Bittereschengewambase (Simaroubaceae). It is widespread in the Neotropics.
  • the extracts used according to the invention are preferably obtained from the wood, leaves, flowers, fruits, particularly preferably from the wood.
  • Extract of Quassia amara can according to known manufacturing processes in variable composition with solvents such. As water, methanol, ethanol, acetone, etc., and mixtures thereof at temperatures from room temperature to 100 ° C under mild to vigorous mixing within 10 min. To 24 hours. Under atmospheric pressure up to 200 bar. For enrichment of effectiveness-determining components further concentration steps can be carried out such.
  • Very preferred according to the invention is an extract obtainable by extraction of Quassia amara wood with water.
  • the commercial product of the extract from Quassia Amara may contain, in addition to extractants, additional solvents to improve the shelf life of the product.
  • additional solvents for example, propylene glycol, 1,3-butylene glycol and pentylene glycol are such antimicrobial solvents.
  • Preferred cosmetic or dermatological compositions according to the invention contain, based on their total weight, from 0.001 to 2.0% by weight, preferably from 0.01 to 0.5% by weight and in particular from 0.05 to 0.2% by weight of pentylene glycol.
  • cosmetic or dermatological agents according to the invention contain, based on their total weight, 0.003 to 6.0% by weight, preferably 0.03 to 1.5% by weight and in particular 0.15 to 0.6% by weight 1 , 3-Butylene glycol.
  • compositions according to the invention with Quassia amara extract exhibit, compared with the middle variant which does not contain Quassia amara extract, much better lightening effect against skin spots and protect the skin more effectively against the appearance of new skin patches.
  • compositions according to the invention contain at least one saturated or unsaturated, linear (C 9 -C 18) -dicarboxylic acid, in particular 8-hexadecene-1,16-dicarboxylic acid and / or 7-tetradecene-1,14-dicarboxylic acid and / or 9 Octadecene-1,18-dicarboxylic acid and / or 6-dodecene-1,12-dicarboxylic acid and / or 5-decene-1,10-dicarboxylic acid and / or decanedioic acid (sebacic acid) and / or nonanedioic acid (azelaic acid), very particularly preferably 8-hexadecene-1,16-dicarboxylic acid.
  • linear (C 9 -C 18) -dicarboxylic acid in particular 8-hexadecene-1,16-dicarboxylic acid and / or 7-tetradecene-1,
  • compositions according to the invention contain, based on their total weight, the saturated or unsaturated, linear (C 9 -C 18) -dicarboxylic acid, in particular the 8-hexadecene-1,16-dicarboxylic acid, in a total amount of 0.01-10% by weight. , preferably 0.05 to 1 wt .-% and in particular 0.1 to 0.5 wt .-%.
  • 8-hexadecene-1,16-dicarboxylic acid (Dioic acid, CAS number 20701-68-2), also referred to as 9-octadecene-1,18-diacid, is a metabolite of yeast cells from selected mutant strains of Candida Strain, using as starting substance a fatty acid of pure vegetable origin, which is converted into the hydroxy fatty acid, which is then oxidized through the stage of fatty acid aldehyde to dicarboxylic acid.
  • 8-hexadecene-1,16-dicarboxylic acid is characterized by the following structure:
  • 8-hexadecene-1,16-dicarboxylic acid is available under the trade name ODA White (INCI name OCTADECENEDIOIC ACID, BHT) from Croda (Sederma).
  • ODA White ICI name OCTADECENEDIOIC ACID, BHT
  • the commercial product has a purity of 100%, wherein the 8-hexadecene-1,16-dicarboxylic acid is present therein as a mixture of the cis and trans isomers and the cis isomer predominates in terms of quantity.
  • the at least one extract of Quassia Amara and the at least one saturated or unsaturated, linear (C9 to C18) dicarboxylic acid are used in specific proportions to one another.
  • Cosmetic or dermatological agents according to the invention are preferred in which the weight ratio of the total content of Quassia Amara extract to the total amount of saturated or unsaturated, linear (C9 to C18) dicarboxylic acid is 1:10 to 5: 1, preferably 1: 5 to 2 : 1 and in particular 1: 3 to 1: 1, is.
  • the compositions according to the invention in order to support the whitening effect, additionally comprise a total of the combination of at least one Quassia Amara extract with at least one saturated or unsaturated, linear (C9- to C18) -dicarboxylic acid, based on the total weight of the compositions according to the invention 0.01 to 5% by weight, preferably 0.1 to 1% by weight, of at least one further skin-lightening substance selected from the group consisting of ascorbic acid, ascorbic acid salts, ascorbic acid glycosides, ascorbic acid glycoside salts, ascorbic acid esters of organic acids, the salts of ascorbic acid esters of organic acids, ascorbic acid esters of inorganic acids, the salts of ascorbic acid esters of inorganic acids, and mixtures of the aforementioned substances, in particular ascorbic acid.
  • ascorbic acid salts the alkali and alkaline earth salts are preferred.
  • Particularly preferred salts of ascorbic acid which can be used according to the invention are sodium hydroascorbate, sodium ascorbate, potassium hydroascorbate, potassium ascorbate, ammonium ascorbate, ammonium hydroascorbate, calcium ascorbate, calcium hydroascorbate, magnesium ascorbate and magnesium hydroascorbate.
  • esters of ascorbic acid can be used.
  • Ascorbyl methanoate, ascorbyl ethanoate, ascorbyl n-propanoate, ascorbyl iso-propanoate, ascorbyl n-butanoate, etc. are particularly preferred among the esters of ascorbic acid.
  • the agents according to the invention contain esters of ascorbic acid with fatty acids, in particular ascorbyl linoleate, ascorbyl oleate, ascorbyloleinate, ascorbyl palmitate, ascorbyl stearate, ascorbyl oleate (6-palmitoyl-L-ascorbic acid) and ascorbyl tetraisopalmitate.
  • inorganic acids can be esterified with ascorbic acid.
  • inorganic esters of ascorbic acid particular preference is given to ascorbyl phosphate.
  • ascorbic acid derivatives with glycosidically bound sugars are inventively used with particular preference.
  • the ascorbyl glucoside has proven to be useful here.
  • compositions according to the invention which contain ascorbyl phosphate and / or ascorbyl glucoside and / or ascorbyl tetraisopalmitate.
  • compositions according to the invention may further comprise at least one conditioning agent selected from the group of vitamins, provitamins or vitamin precursors.
  • vitamins, provitamins or vitamin precursors are in the inventive compositions in an amount of 0.1 to 10 wt .-%, preferably 0.2 to 5 wt .-% and in particular 0.5 to 1 wt .-%, each based on the total weight of the funds, contain.
  • such vitamins, pro-vitamins and vitamin precursors are preferred, which are usually assigned to groups A, B, F and H.
  • vitamin A includes retinol (vitamin A1) and 3,4-didehydroretinol (vitamin A2).
  • the ⁇ -carotene is the provitamin of retinol.
  • vitamin A component according to the invention for example, vitamin A acid and its esters, vitamin A aldehyde and vitamin A alcohol and its esters such as the palmitate and the acetate into consideration.
  • vitamin F is usually understood as meaning essential fatty acids, in particular linoleic acid, linolenic acid and arachidonic acid.
  • Vitamin H is the compound (3aS, 4S, 6aR) -2-oxohexahydrothienol [3,4-d] -imidazole-4-valeric acid, for which, however, the trivial name biotin has meanwhile prevailed.
  • UV filters to be used according to the invention are not subject to any general restrictions with regard to their structure and their physical properties. On the contrary, all UV filters which can be used in the cosmetics sector and whose absorption maximum lies in the UVA (315-400 nm), in the UVB (280-315 nm) or in the UVC ( ⁇ 280 nm) range are suitable.
  • the UVA, UVB and UVC filters can be used individually or in mixtures. UV filters with an absorption maximum in the UVB range, in particular in the range from about 280 to about 300 nm, are particularly preferred.
  • the organic UV filters preferred according to the invention are selected from the derivatives of dibenzoylmethane, cinnamic acid esters, diphenylacrylic esters, benzophenone, camphor, p-aminobenzoic acid esters, o-aminobenzoic acid esters, salicylic acid esters, benzimidazoles, symmetrically or unsymmetrically substituted 1,3,5-triazines, monomeric and oligomeric 4,4-Diarylbutadienecarboxylic acid esters and carboxamides, ketotricyclo (5.2.1.0) decane, benzalmalonic acid esters, Benzoxazole and any mixtures of the components mentioned.
  • the organic UV filters can be oil-soluble or water-soluble.
  • the benzoxazole derivatives are advantageously present in dissolved form in the cosmetic preparations according to the invention. However, it may also be advantageous if the benzoxazole derivatives are present in a pigmentary, ie undissolved form, for example in particle sizes of from 10 nm to 300 nm.
  • oil-soluble UV filters are 1- (4-tert-butylphenyl) -3- (4'-methoxyphenyl) propane-1,3-dione (Parsol ® 1789), 1-phenyl-3- (4'- isopropylphenyl) -propane-1,3-dione, 3- (4'-methylbenzylidene) -D, L-camphor, 4- (dimethylamino) benzoic acid 2-ethylhexyl ester, 4- (dimethylamino) benzoic acid 2-octyl ester, 4 - (dimethylamino) benzoic acid ester, 4-methoxycinnamic acid 2-ethylhexyl ester, 4-methoxycinnamic acid propyl ester, 4-methoxycinnamic acid isopentyl ester, 2-cyano-3,3-phenylcinnamic acid 2-ethylhexyl ester (o
  • 2,4-bis - ⁇ [4- (2-ethyl-hexyloxy) -2-hydroxy] -phenyl ⁇ -6- (4-methoxyphenyl) -1,3,5-triazine (INCI: bis-ethylhexyloxyphenol methoxyphenyl triazine, available under the name Tinosorb S from CIBA), dioctylbutylamidotriazone (INCI: Diethylhexyl Butamido Triazone, available under the name Uvasorb HEB from Sigma 3V ®), 2,4,6-trianilino- (p-carbo-2'-ethyl- 1'-hexyloxy) -1,3,5-triazine (ethylhexyl triazone, Uvinul ® T 150), 2- [4,6-bis (2,4-dimethylphenyl) -1,3,5-triazin-2-yl ] -5- (octyl
  • Preferred water-soluble UV filters are 2-phenylbenzimidazole-5-sulfonic acid, phenylene-1,4-bis (2-benzimidazyl) -3,3'-5,5'-tetrasulfonic acid and their alkali metal, alkaline earth metal, ammonium, Alkylammonium, Alkanolammonium- and Glucammoniumsalze, in particular the sulfonic acid itself with the INCI name Phenylbenzimidazole Sulfonic Acid (CAS No.
  • Inorganic pigments can also be used according to the invention as UV filters.
  • Preferred inorganic pigments are metal oxides and / or other sparingly water-soluble or insoluble metal compounds, for example carbonates, sulfates, etc.
  • the inorganic pigments may have a maximum average particle diameter of 200 microns and from the oxides of silicon, titanium, iron, zinc, zirconium, magnesium, cerium and bismuth, boron nitride, mica, fluorspar and water-insoluble pearlescent pigments containing at least one inorganic and / or or organic compound may be selected.
  • Preferred inorganic pigments have a diameter of 1 to 100 .mu.m, more preferably 1 to 50 .mu.m, and most preferably 1 to 10 .mu.m.
  • the pigments can be both colored and colorless.
  • the preferred pigments are selected from the oxides of silicon, titanium, zinc and iron, as well as bismuth oxychloride. Further preferred pigments according to the invention are mica and pearlescent pigments.
  • the said inorganic pigments may be coated.
  • the coating can be carried out with the aid of inorganic and / or organic compounds. According to the invention, preference is given to inorganic pigments which have an inorganic coating.
  • Preferred pigments of this type are selected from silica particles coated with titanium dioxide and / or iron oxides.
  • a particularly preferred pigment of this type is the commercial product Ronasphere® LDP from Merck KGaA. This product is a spherical silica particle coated with titanium dioxide and iron oxide. Ronasphere® LDP has a refractive index that is similar to the refractive index of the skin.
  • inorganic-coated mica pigments which have no pearlescence.
  • inorganic-coated inorganic pigments are mica pigments which are coated with titanium dioxide in various layer thicknesses, for example the product RonaFlair® Extender W from Merk KGaA. The named product had average particle diameters of 3 to 8 ⁇ m. Also preferred are mica particles having a coating of metal oxide mixture.
  • Other pigments which are suitable according to the invention are inorganic-coated inorganic pigments whose coating has a proportion of 0.1-5% by weight of tin oxide.
  • inorganic pigments coated with organic substances examples include aluminum stearate coated titanium dioxide pigments, dimethylpolysiloxane (dimethicone) coated zinc oxide, dimethicone coated boron nitride, a mixture of dimethylpolysiloxane and silica gel (simethicone) and alumina hydrate (alumina) coated titania, octylsilanol coated titania or spherical polyalkylsesquisiloxane particles ,
  • the agents according to the invention comprise at least one metal oxide, preferably a metal oxide as skin-lightening active ingredient.
  • cosmetic or dermatological agents according to the invention which contain, based on their total weight, a total of 0.01 to 5 wt .-%, preferably 0.1 to 3 wt .-% metal oxide, preferably metal oxide as skin-lightening agent.
  • Titanium dioxide is preferably usable according to the invention.
  • compositions of the invention contain the respective active ingredients in a cosmetically acceptable carrier.
  • This cosmetic carrier is preferably aqueous, alcoholic, aqueous-alcoholic or aqueous-glycolic.
  • Such carriers are, for example, creams, emulsions, gels or surfactant-containing foaming solutions, such as shower gels or other preparations which are suitable for use on the skin.
  • An aqueous carrier contains in According to the invention preferably at least 40 wt .-%, particularly preferably at least 50 wt .-% water.
  • Cosmetic agents preferred according to the invention are characterized in that they contain 10 to 80% by weight, preferably 20 to 75% by weight, more preferably 30 to 70% by weight, even more preferably 35 to 100% by weight, based on the total weight of the ready-to-use agent 60 wt .-% and in particular 40 to 60 wt .-% water.
  • aqueous-alcoholic carriers are water-containing compositions containing from 3 to 70% by weight, preferably from 10 to 60% by weight, particularly preferably from 15 to 40% by weight, of a monohydric C 2 -C 4 -alcohol. especially ethanol, to understand.
  • aqueous-glycolic carriers are water-containing compositions containing from 3 to 70% by weight, preferably from 10 to 60% by weight, particularly preferably from 15 to 40% by weight, of at least one bivalent or polyvalent C 2 C9 alcohol or at least one water-soluble polyethylene glycol having 3 to 20 ethylene oxide units, in particular selected from 1,2-propylene glycol, 2-methyl-1,3-propanediol, glycerol, 1,2-butylene glycol, 1,3-butylene glycol , 1,4-butylene glycol, pentylene glycols such as 1,2-pentanediol and 1,5-pentanediol, hexanediols such as 1,6-hexanediol, hexanetriols such as 1,2,6-hexanetriol, 1,2-octanediol, 1,8-octanediol , Dipropylene glycol, tripropylene glycol, 1,2-prop
  • compositions of the invention may additionally contain other organic solvents such as, for example, methoxybutanol, ethyl diglycol, 1,2-propylene glycol, 2-methyl-1,3-propanediol, n-propanol, n-butanol, n-butylene glycol, glycerol, diethylene glycol monoethyl ether and diethylene glycol mono-n butyl ether. Preference is given to all water-soluble organic solvents.
  • compositions according to the invention can be formulated in all dosage forms suitable for topical application to the skin.
  • Preferred dosage forms are a solution, a water-in-oil (W / O) type emulsion, an oil-in-water (O / W) type emulsion, a multiple emulsion, for example, water-in-oil-in type Water (W / O / W) or oil-in-water-in-oil (O / W / O), a hydrodispersion, a lipodispersion, a gel, a hydrodispersion gel, a lipodispersion gel, a solid stick, a gel patch (Gelpatch ), a patch, a cataplasm, drug-containing liposomes or a transdermal therapeutic system.
  • Low-viscous or medium-viscosity dosage forms may also be packaged in a propellant-free pump or spray dispenser or together with a propellant in an aerosol container.
  • the ready-to-use agents according to the invention may contain further active ingredients, auxiliaries and additives.
  • the agents contain at least one thickener.
  • the agents are provided as flowable preparations.
  • Flowable in the context of the present application are compositions which are pourable and may have viscosities of from 10 mPa.s up to 250,000 mPa.s (20 ° C.). The viscosity can be measured by conventional standard methods (for example Brookfield LVT-II viscosimeter at 20 rpm and 20 ° C., spindle 3) and is preferably in the range from 50 to 50 000 mPa ⁇ s.
  • Preferred agents have viscosities of from 1000 to 30,000 mPas, with values of from 5,000 to 20,000 mPas being particularly preferred.
  • emulsions As in the form of a cream, a lotion or a cosmetic milk, are advantageous and contain z.
  • the agents according to the invention preferably contain the emulsifiers in amounts of from 0.1 to 30% by weight, in particular from 3 to 15% by weight, based on the total agent.
  • the agents according to the invention may preferably contain at least one nonionic emulsifier having an HLB value of 8 to 18.
  • Nonionic emulsifiers having an HLB value of 10 to 15 may be particularly preferred according to the invention.
  • compositions according to the invention are suitable for lightening the skin and can be used accordingly.
  • the skin can be locally limited (for example freckles, age spots or Friedpigmentmaschineen) or large (for skin lightening) to be treated.
  • Another object of the present invention is the non-therapeutic, cosmetic use of cosmetic and dermatological agents according to the invention for the treatment of postinflammatory hyperpigmentation.
  • compositions of the invention according to formula 66 were tested in a use test under dermatological control on 50 subjects with age spots on the face.
  • the test subjects should use the funds for facial care at least twice a day for a total of 4 weeks.
  • the dermatological use test of the compositions according to the invention in comparison to the middle variant which does not contain Quassia amara extract shows that the compositions according to the invention with Quassia amara extract show much better whitening effects against skin spots and protect the skin more effectively against the appearance of new skin patches.

Abstract

Kosmetische oder dermatologische Mittel, enthaltend eine Kombination aus mindestens einem der unter a) und mindestens einem der unter b) aufgeführten Wirkstoffe: a) Extrakt aus Quassia Amara; b) gesättigte oder ungesättigte, lineare (C9- bis C18)-Dicarbonsäure, insbesondere 8-Hexadecen-1,16-dicarbonsäure und/oder 7-Tetradecen-1, 14-dicarbonsäure und/oder 9-Octadecen-1,18-dicarbonsäure und/oder 6-Dodecen-1,12-dicarbonsäure und/oder 5-Decen-1,10-dicarbonsäure und/oder Decandisäure (Sebacinsäure) und/oder Nonandisäure (Azelainsäure), ganz besonders bevorzugt 8-Hexadecen-1,16-dicarbonsäure. eignen sich zur kosmetischen und topischen dermatologischen Hautaufhellung oder zur Verhinderung der Hautbräunung, insbesondere der durch UV-Strahlung hervorgerufenen Hautbräunung, sowie zur Aufhellung von Altersflecken oder Sommersprossen.Cosmetic or dermatological compositions containing a combination of at least one of the active substances listed under a) and at least one of the substances listed under b): a) Extract from Quassia Amara; b) saturated or unsaturated, linear (C9 to C18) dicarboxylic acid, in particular 8-hexadecene-1,16-dicarboxylic acid and / or 7-tetradecene-1, 14-dicarboxylic acid and / or 9-octadecene-1,18-dicarboxylic acid and / or 6-dodecene-1,12-dicarboxylic acid and / or 5-decene-1,10-dicarboxylic acid and / or decanedioic acid (sebacic acid) and / or nonanedioic acid (azelaic acid), very particularly preferably 8-hexadecene-1,16- dicarboxylic acid. are suitable for cosmetic and topical dermatological skin whitening or to prevent tanning of the skin, in particular the skin tanning caused by UV radiation, as well as for lightening age spots or freckles.

Description

Die vorliegende Erfindung betrifft kosmetische oder dermatologische Mittel zur kosmetischen und topischen dermatologischen Hautaufhellung oder zur Verhinderung der Hautbräunung, insbesondere der durch UV-Strahlung hervorgerufenen Hautbräunung, sowie zur Aufhellung von Altersflecken oder Sommersprossen. Die vorliegende Erfindung betrifft weiterhin die Verwendung dieser Mittel und Verfahren unter Einsatz dieser Mittel.The present invention relates to cosmetic or dermatological compositions for the cosmetic and topical dermatological skin whitening or for the prevention of tanning of the skin, in particular the skin tanning caused by UV radiation, and for the lightening of age spots or freckles. The present invention further relates to the use of these agents and methods using these agents.

Die Pigmentierung der Haut erfolgt durch Melanozyten, welche in der untersten Schicht der Epidermis neben den Basalzellen als je nach Hauttyp entweder vereinzelt oder gehäuft auftretende pigmentbildende Zellen vorzufinden sind. Melanozyten enthalten Melanosomen, in denen Melanin gebildet wird. Durch verschiedene chemische und/oder physikalische Einflüsse, insbesondere durch UV-Strahlung, wird verstärkt Melanin gebildet. Dieses wird über die Keratinozyten in die Corneozyten (Hornschicht) transportiert und führt zu einer bräunlichen bis braun-schwarzen Hautfarbe. Melanin wird als Endstufe eines oxidativen Prozesses gebildet, in welchem Tyrosin unter Mitwirkung der Enzyms Tyrosinase über mehrere Zwischenstufen zu den braun bis braunschwarzen Eumelaninen (DHICA- und DHI-Melanin) bzw. unter Beteiligung von schwefelhaltigen Verbindungen zum rötlichen Phäomelanin umgewandelt wird. Die Melaninbildung - und damit Hautfarbe - unterliegt äußeren Einflüssen und kann neben erwünschten Effekten ("gesunde Bräune") auch zu unerwünschten Erscheinungen führen. So kann z.B. UV-Strahlung zu Sommersprossen führen. Fehlpigmentierungen können auch aufgrund genetischer Disposition, Wundheilung bzw. -vernarbung oder Hautalterung ("Altersflecken") auftreten. Da der Prozess der Desquamation (oberflächliche Loslösung von Zellen oder Zellgruppen aus ihrem epithelialen Verband) einen beständigen Verlust an Melanin beinhaltet, kann eine Aufhellung der Haut durch Inhibierung der Neusynthese von Melanin erreicht werden.The pigmentation of the skin is carried out by melanocytes, which are found in the lowest layer of the epidermis in addition to the basal cells as either isolated or frequently occurring pigment-forming cells depending on the skin type. Melanocytes contain melanosomes in which melanin is formed. Through various chemical and / or physical influences, in particular by UV radiation, melanin is increasingly formed. This is transported via the keratinocytes into the corneocytes (horny layer) and leads to a brownish to brown-black skin color. Melanin is formed as the final stage of an oxidative process in which tyrosine is converted by means of the enzyme tyrosinase via several intermediates to the brown to brown-black eumelanins (DHICA and DHI melanin) or with the involvement of sulfur-containing compounds to the reddish phaeomelanin. Melanin formation - and thus skin color - is subject to external influences and, in addition to desirable effects ("healthy tan"), can also lead to undesired symptoms. Thus, e.g. UV radiation lead to freckles. Malignant pigmentation may also occur due to genetic disposition, wound healing or scarring, or skin aging ("age spots"). Since the process of desquamation (superficial detachment of cells or cell groups from their epithelial dressing) involves a constant loss of melanin, lightening of the skin can be achieved by inhibiting the new synthesis of melanin.

Altersflecken stellen ein Zeichen der Hautalterung dar, das einer speziellen Behandlung bedarf. Bei Altersflecken handelt es sich nicht um eine intensivere Pigmentierung der Haut, sondern konkret um Anhäufungen des bräunlich-wachsartigen Pigments Lipofuscin (auch Alters- oder Abnutzungspigment), das als Endprodukt aus der Oxidation von ungesättigten Fettsäuren der Zellmembranen entsteht. Die Lysosomen sind nicht mehr imstande, den Stoff vollständig abzubauen. So bleibt er als Fleck zurück.Age spots are a sign of aging that requires special treatment. Age spots are not a more intensive pigmentation of the skin, but actually accumulations of the brownish-waxy pigment lipofuscin (also age or wear pigment), which is the end product of the oxidation of unsaturated fatty acids of cell membranes. The lysosomes are no longer able to completely degrade the substance. So he stays back as a stain.

Wirksame kosmetische Mittel zur Hautaufhellung sind bekannt. Diese enthalten als Wirkstoff jedoch zumeist Hydrochinon oder Kojisäure (zur Inhibierung der Tyrosinase). Beide Substanzen sind mutagen und sollten daher nicht über längere Zeiträume verwendet werden. Hautkosmetische Mittel zur Behandlung von Altersflecken werden beispielsweise in der europäischen Patentanmeldung EP 2163238 A2 beschrieben.Effective cosmetic skin whitening agents are known. However, these usually contain as active ingredient hydroquinone or kojic acid (for the inhibition of tyrosinase). Both substances are mutagenic and should therefore not be used for prolonged periods. Skin cosmetic agents for the treatment of age spots are described, for example, in the European patent application EP 2163238 A2 described.

Es bestand nach wie vor die Aufgabe, lagerstabile hautaufhellende kosmetische oder dermatologische Mittel zur Verfügung zu stellen, die hochwirksam, auch unter UV-Bestrahlung (Sonnenlicht) anwendbar und möglichst auf Naturstoffen basiert sind. Darüber hinaus sollten weitere positive Effekte auf älterer Haut ermöglicht werden, z.B Hautstraffung und/oder Reduktion der Hautfalten.It was still the task of providing storage-stable skin-lightening cosmetic or dermatological agents which are highly effective, also applicable under UV irradiation (sunlight) and, if possible, based on natural substances. In addition, further positive effects on older skin should be made possible, for example skin tightening and / or reduction of the skin folds.

Es hat sich überraschenderweise gezeigt, dass die Kombination von mindestens einem Extrakt aus Quassia Amara, mit mindestens einer Dicarbonsäure, ausgewählt aus 9-Octadecen-1,18-dicarbon-säure, 8-Hexadecen-1,16-dicarbonsäure, 7-Tetradecen-1,14-dicarbonsäure, 6-Dodecen-1,12-dicarbonsäure, 5-Decen-1,10-dicarbonsäure, Sebacinsäure und Azelainsäure sowie Mischungen dieser Dicarbonsäuren, zu einer besonders guten Aufhellung der Hautfarbe führt, sowohl bei großflächiger Anwendung auf der Haut als auch bei lokaler Anwendung auf Pigmentstörungen wie Altersflecken.It has surprisingly been found that the combination of at least one extract of Quassia Amara, with at least one dicarboxylic acid selected from 9-octadecene-1,18-dicarboxylic acid, 8-hexadecene-1,16-dicarboxylic acid, 7-tetradecene 1,14-dicarboxylic acid, 6-dodecene-1,12-dicarboxylic acid, 5-decene-1,10-dicarboxylic acid, sebacic acid and azelaic acid and mixtures of these dicarboxylic acids, leading to a particularly good lightening of the skin color, both in large-scale application to the skin as well as local application to pigmentary disorders such as age spots.

Ein erster Gegenstand der vorliegenden Erfindung sind daher kosmetische oder dermatologische Mittel, enthaltend eine Kombination aus mindestens einem der unter a) und mindestens einem der unter b) aufgeführten Wirkstoffe:

  1. a) Extrakt aus Quassia Amara;
  2. b) gesättigte oder ungesättigte, lineare (C9- bis C18)-Dicarbonsäure, insbesondere 8-Hexadecen-1,16-dicarbonsäure und/oder 7-Tetradecen-1, 14-dicarbonsäure und/oder 9-Octadecen-1,18-dicarbonsäure und/oder 6-Dodecen-1,12-dicarbonsäure und/oder 5-Decen-1,10-dicarbonsäure und/oder Decandisäure (Sebacinsäure) und/oder Nonandisäure (Azelainsäure), ganz besonders bevorzugt 8-Hexadecen-1,16-dicarbonsäure.
A first subject of the present invention are therefore cosmetic or dermatological compositions comprising a combination of at least one of the active substances listed under a) and at least one of the substances listed under b):
  1. a) Extract from Quassia Amara;
  2. b) saturated or unsaturated, linear (C9 to C18) dicarboxylic acid, in particular 8-hexadecene-1,16-dicarboxylic acid and / or 7-tetradecene-1, 14-dicarboxylic acid and / or 9-octadecene-1,18-dicarboxylic acid and / or 6-dodecene-1,12-dicarboxylic acid and / or 5-decene-1,10-dicarboxylic acid and / or decanedioic acid (sebacic acid) and / or nonanedioic acid (azelaic acid), very particularly preferably 8-hexadecene-1,16- dicarboxylic acid.

Die erfindungsgemäßen Mittel enthalten als erste obligatorische Komponente, bezogen auf das Gesamtgewicht der erfindungsgemäßen Mittel, insgesamt 0,001 bis 2,0 Gew.-%, vorzugsweise 0,01 bis 0,5 Gew.-% und insbesondere 0,05 bis 0,2 Gew.-% mindestens eines Extraktes aus Quassia Amara.The compositions according to the invention contain as the first obligatory component, based on the total weight of the compositions according to the invention, a total of from 0.001 to 2.0% by weight, preferably from 0.01 to 0.5% by weight and in particular from 0.05 to 0.2% by weight .-% of at least one extract from Quassia Amara.

Der Quassia amara, Brasilianischer Quassiabaum, Quassiabaum, Quassiaholzbaum, Bitterquassia oder wie einige andere Arten auch Bitterholz genannt, ist eine Pflanzenart in der Familie der Bittereschengewächse (Simaroubaceae). Sie ist in der Neotropis weit verbreitet. Die erfindungsgemäß eingesetzten Extrakte werden vorzugsweise aus dem Holz, Blättern, Blüten, Früchten, besonders bevorzugt aus dem Holz gewonnen.The Quassia amara, Brazilian Quassia tree, Quassia tree, Quassia tree, Bitter quassia or as some other species also called Bitter wood, is a plant species in the family Bittereschengewächse (Simaroubaceae). It is widespread in the Neotropics. The extracts used according to the invention are preferably obtained from the wood, leaves, flowers, fruits, particularly preferably from the wood.

Extrakt aus Quassia amara können nach bekannten Herstellungsverfahren in variabler Zusammensetzung mit Lösungsmitteln wie z. B. Wasser, Methanol, Ethanol, Aceton, etc., und deren Gemische bei Temperaturen von Raumtemperatur bis 100 °C unter gelinder bis heftiger Durchmischung innerhalb von 10 Min. bis 24 Std. unter Normaldruck bis zu 200 bar erhalten werden. Zur Anreicherung wirksamkeitsbestimmender Komponenten können weitere Konzentrierungsschritte durchgeführt werden wie z. B. flüssig-flüssig-Verteilung mit z. B. 1-Butanol/Wasser oder Ethylacetat/Wasser, Adsorption-Desorption an Ionenaustauscher, LH20, HP20 und andere Harze oder chromatographische Abtrennungen über RP18, Kieselgel, etc.. Falls die Weiterverarbeitung zu Trockenextrakten erwünscht ist, erfolgt diese nach an sich bekannten Verfahren durch Abziehen des Lösungsmittels bei erhöhter Temperatur und / oder reduziertem Druck. Die Angaben zum Gewichtsanteil von Quassia Amara am Gesamtgewicht der erfindungsgemäßen Mittel beziehen sich auf die Trockenmasse des Extraktes.Extract of Quassia amara can according to known manufacturing processes in variable composition with solvents such. As water, methanol, ethanol, acetone, etc., and mixtures thereof at temperatures from room temperature to 100 ° C under mild to vigorous mixing within 10 min. To 24 hours. Under atmospheric pressure up to 200 bar. For enrichment of effectiveness-determining components further concentration steps can be carried out such. B. liquid-liquid distribution with z. B. 1-butanol / water or ethyl acetate / water, adsorption-desorption on ion exchanger, LH20, HP20 and other resins or chromatographic separations over RP18, silica gel, etc .. If further processing to dry extracts is desired, this is carried out according to known methods by stripping off the solvent at elevated temperature and / or reduced pressure. The data on the weight fraction of Quassia Amara in the total weight of the compositions of the invention are based on the dry matter of the extract.

Erfindungsgemäß ganz bevorzugt ist ein Extrakt, der durch Extraktion von Quassia amara Holz mit Wasser erhältlich ist.Very preferred according to the invention is an extract obtainable by extraction of Quassia amara wood with water.

Das Handelsprodukt des Extraktes aus Quassia Amara kann außer Extraktionsmittel noch zusätzliche Lösungsmittel zur Verbesserung der Haltbarkeit des Produkts enthalten. Propylenglycol, 1,3 - Butylenglycol und Pentylenglycol sind beispielweise solche antimikrobiellen Lösungsmittel.The commercial product of the extract from Quassia Amara may contain, in addition to extractants, additional solvents to improve the shelf life of the product. For example, propylene glycol, 1,3-butylene glycol and pentylene glycol are such antimicrobial solvents.

Bevorzugte erfindungsgemäße kosmetische oder dermatologische Mittel enthalten, bezogen auf ihr Gesamtgewicht, 0,001 bis 2,0 Gew.-%, vorzugsweise 0,01 bis 0,5 Gew.-% und insbesondere 0,05 bis 0,2 Gew.-% Pentylenglycol.Preferred cosmetic or dermatological compositions according to the invention contain, based on their total weight, from 0.001 to 2.0% by weight, preferably from 0.01 to 0.5% by weight and in particular from 0.05 to 0.2% by weight of pentylene glycol.

Weitere bevorzugte erfindungsgemäße kosmetische oder dermatologische Mittel enthalten, bezogen auf ihr Gesamtgewicht, 0,003 bis 6,0 Gew.-%, vorzugsweise 0,03 bis 1,5 Gew.-% und insbesondere 0,15 bis 0,6 Gew.-% 1,3 - Butylenglycol.Further preferred cosmetic or dermatological agents according to the invention contain, based on their total weight, 0.003 to 6.0% by weight, preferably 0.03 to 1.5% by weight and in particular 0.15 to 0.6% by weight 1 , 3-Butylene glycol.

Die erfindungsgemäßen Mittel mit Extrakt aus Quassia amara zeigen im Vergleich zur Mittelvariante, die kein Quassia amara Extrakt enthält, viel bessere Aufhellungseffekt gegen Hautflecken und schützten die Haut wirksamer gegen das Auftreten neuer Hautflecken.The compositions according to the invention with Quassia amara extract exhibit, compared with the middle variant which does not contain Quassia amara extract, much better lightening effect against skin spots and protect the skin more effectively against the appearance of new skin patches.

Als zweite obligatorische Komponente enthalten die erfindungsgemäßen Mittel mindestens eine gesättigte oder ungesättigte, lineare (C9- bis C18)-Dicarbonsäure, insbesondere 8-Hexadecen-1,16-dicarbonsäure und/oder 7-Tetradecen-1,14-dicarbonsäure und/oder 9-Octadecen-1,18-dicarbonsäure und/oder 6-Dodecen-1,12-dicarbonsäure und/oder 5-Decen-1,10-dicarbonsäure und/oder Decandisäure (Sebacinsäure) und/oder Nonandisäure (Azelainsäure), ganz besonders bevorzugt 8-Hexadecen-1,16-dicarbonsäure.As a second obligatory component, the compositions according to the invention contain at least one saturated or unsaturated, linear (C 9 -C 18) -dicarboxylic acid, in particular 8-hexadecene-1,16-dicarboxylic acid and / or 7-tetradecene-1,14-dicarboxylic acid and / or 9 Octadecene-1,18-dicarboxylic acid and / or 6-dodecene-1,12-dicarboxylic acid and / or 5-decene-1,10-dicarboxylic acid and / or decanedioic acid (sebacic acid) and / or nonanedioic acid (azelaic acid), very particularly preferably 8-hexadecene-1,16-dicarboxylic acid.

Die erfindungsgemäßen Mittel enthalten, bezogen auf ihr Gesamtgewicht, die gesättigte oder ungesättigte, lineare (C9- bis C18)-Dicarbonsäure, insbesondere die 8-Hexadecen-1,16-dicarbonsäure, in einer Gesamtmenge von 0,01 - 10 Gew.-%, vorzugsweise 0,05 bis 1 Gew.-% und insbesondere 0,1 bis 0,5 Gew.-%.The compositions according to the invention contain, based on their total weight, the saturated or unsaturated, linear (C 9 -C 18) -dicarboxylic acid, in particular the 8-hexadecene-1,16-dicarboxylic acid, in a total amount of 0.01-10% by weight. , preferably 0.05 to 1 wt .-% and in particular 0.1 to 0.5 wt .-%.

8-Hexadecen-1,16-dicarbonsäure (Dioic acid, CAS-Nummer 20701-68-2), die auch als 9-Octadecen-1,18-disäure bezeichnet wird, ist ein Stoffwechselprodukt von Hefezellen aus selektierten Mutanten-Stämmen des Candida Stammes, wobei als Ausgangssubstanz eine Fettsäure rein pflanzlichen Ursprungs dient, die in die Hydroxyfettsäure umgesetzt wird, welche anschließend über die Stufe des Fettsäurealdehyd zur Dicarboxysäure oxidiert wird. 8-Hexadecen-1,16-dicarbonsäure ist durch folgende Struktur gekennzeichnet:

Figure imgb0001
8-hexadecene-1,16-dicarboxylic acid (Dioic acid, CAS number 20701-68-2), also referred to as 9-octadecene-1,18-diacid, is a metabolite of yeast cells from selected mutant strains of Candida Strain, using as starting substance a fatty acid of pure vegetable origin, which is converted into the hydroxy fatty acid, which is then oxidized through the stage of fatty acid aldehyde to dicarboxylic acid. 8-hexadecene-1,16-dicarboxylic acid is characterized by the following structure:
Figure imgb0001

8-Hexadecen-1,16-dicarbonsäure ist unter dem Handelsnamen ODA White (INCI-Bezeichnung OCTADECENEDIOIC ACID, BHT) von Croda (Sederma) erhältlich. Das Handelsprodukt besitzt eine Reinheit von 100%, wobei die 8- Hexadecen-1,16-dicarbonsäure darin als Gemisch des cis-und trans- Isomeren vorliegt und das cis-Isomere mengenmäßig überwiegt.8-hexadecene-1,16-dicarboxylic acid is available under the trade name ODA White (INCI name OCTADECENEDIOIC ACID, BHT) from Croda (Sederma). The commercial product has a purity of 100%, wherein the 8-hexadecene-1,16-dicarboxylic acid is present therein as a mixture of the cis and trans isomers and the cis isomer predominates in terms of quantity.

Vorzugsweise werden der mindestens eine Extrakt aus Quassia Amara und die mindestens eine gesättigte oder ungesättigte, lineare (C9- bis C18)-Dicarbonsäure in bestimmten Mengenverhältnissen zueinander eingesetzt. Hier sind erfindungsgemäße kosmetische oder dermatologische Mittel bevorzugt, bei denen das Gewichtsverhältnis des Gesamtgehalts an Extrakt aus Quassia Amara zur Gesamtmenge der gesättigten oder ungesättigten, linearen (C9- bis C18)-Dicarbonsäure 1 : 10 bis 5: 1, vorzugsweise 1 : 5 bis 2 : 1 und insbesondere 1 : 3 bis 1 : 1, beträgt.Preferably, the at least one extract of Quassia Amara and the at least one saturated or unsaturated, linear (C9 to C18) dicarboxylic acid are used in specific proportions to one another. Cosmetic or dermatological agents according to the invention are preferred in which the weight ratio of the total content of Quassia Amara extract to the total amount of saturated or unsaturated, linear (C9 to C18) dicarboxylic acid is 1:10 to 5: 1, preferably 1: 5 to 2 : 1 and in particular 1: 3 to 1: 1, is.

Bei der Bestimmung des Gewichtsverhältnisses kommt nur Trockenmasse des Extraktes aus Quassia Amara in Betracht.When determining the weight ratio only dry matter of the extract from Quassia Amara is considered.

In einer bevorzugten Ausführungsform enthalten die erfindungsgemäßen Mittel, zur Unterstützung der aufhellenden Wirkung der Kombination von mindestens einem Extrakt aus Quassia Amara mit mindestens einer gesättigten oder ungesättigten, linearen (C9- bis C18)-Dicarbonsäure, bezogen auf das Gesamtgewicht der erfindungsgemäßen Mittel, zusätzlich insgesamt 0,01 bis 5 Gew.-%, vorzugsweise 0,1 bis 1 Gew.-%, an mindestens einer weiteren hautaufhellenden Substanz, die ausgewählt ist aus der Gruppe, bestehend aus Ascorbinsäure, Ascorbinsäuresalzen, Ascorbinsäureglycosiden, Ascorbinsäureglycosidsalzen, Ascorbinsäureestern von organischen Säuren, den Salzen der Ascorbinsäureester von organischen Säuren, Ascorbinsäureestern von anorganischen Säuren, den Salzen der Ascorbinsäureester von anorganischen Säuren, sowie Mischungen der vorgenannten Substanzen, insbesondere Ascorbinsäure.In a preferred embodiment, the compositions according to the invention, in order to support the whitening effect, additionally comprise a total of the combination of at least one Quassia Amara extract with at least one saturated or unsaturated, linear (C9- to C18) -dicarboxylic acid, based on the total weight of the compositions according to the invention 0.01 to 5% by weight, preferably 0.1 to 1% by weight, of at least one further skin-lightening substance selected from the group consisting of ascorbic acid, ascorbic acid salts, ascorbic acid glycosides, ascorbic acid glycoside salts, ascorbic acid esters of organic acids, the salts of ascorbic acid esters of organic acids, ascorbic acid esters of inorganic acids, the salts of ascorbic acid esters of inorganic acids, and mixtures of the aforementioned substances, in particular ascorbic acid.

Unter Ascorbinsäuresalzen sind die Alkali- und Erdalkalisalze bevorzugt. Besonders bevorzugte Salze der Ascorbinsäure, die erfindungsgemäß eingesetzt werden können, sind Natriumhydroascorbat, Natriumascorbat, Kaliumhydroascorbat, Kaliumascorbat, Ammoniumascorbat, Ammoniumhydroascorbat, Calciumascorbat, Calciumhydroascorbat, Magnesiumascorbat und Magnesiumhydroascorbat.Among ascorbic acid salts, the alkali and alkaline earth salts are preferred. Particularly preferred salts of ascorbic acid which can be used according to the invention are sodium hydroascorbate, sodium ascorbate, potassium hydroascorbate, potassium ascorbate, ammonium ascorbate, ammonium hydroascorbate, calcium ascorbate, calcium hydroascorbate, magnesium ascorbate and magnesium hydroascorbate.

Mit besonderem Vorzug können auch die Ester der Ascorbinsäure eingesetzt werden. Unter den Estern der Ascorbinsäure sind insbesondere Ascorbylmethanoat, Ascorbylethanoat, Ascorbyl-n-propanoat, Ascorbyl-iso-propanoat, Ascorbyl-n-butanoat, usw. bevorzugt. Mit besonderem Vorzug enthalten die erfindungsgemäßen Mittel Ester von Ascorbinsäure mit Fettsäuren, insbesondere Ascorbyllinoleat, Ascorbyloleat, Ascorbyloleinat, Ascorbylpalmitat, Ascorbylstearat, Ascorbyloleat (6-Palmitoyl-L-ascorbinsäure) und Ascorbyltetraisopalmitat.With particular preference, the esters of ascorbic acid can be used. Ascorbyl methanoate, ascorbyl ethanoate, ascorbyl n-propanoate, ascorbyl iso-propanoate, ascorbyl n-butanoate, etc. are particularly preferred among the esters of ascorbic acid. With particular preference the agents according to the invention contain esters of ascorbic acid with fatty acids, in particular ascorbyl linoleate, ascorbyl oleate, ascorbyloleinate, ascorbyl palmitate, ascorbyl stearate, ascorbyl oleate (6-palmitoyl-L-ascorbic acid) and ascorbyl tetraisopalmitate.

Auch "anorganische" Säuren können mit Ascorbinsäure verestert werden. Unter den "anorganischen" Estern der Ascorbinsäure ist insbesondere das Ascorbylphosphat bevorzugt.Also "inorganic" acids can be esterified with ascorbic acid. Among the "inorganic" esters of ascorbic acid, particular preference is given to ascorbyl phosphate.

Auch Ascorbinsäurederivate mit glycosidisch gebundenen Zuckern sind erfindungsgemäß mit besonderem Vorzug einsetzbar. Bewährt hat sich hier insbesondere das Ascorbylglucosid.Also ascorbic acid derivatives with glycosidically bound sugars are inventively used with particular preference. In particular, the ascorbyl glucoside has proven to be useful here.

Bevorzugt sind erfindungsgemäße kosmetische oder dermatologische Mittel, die Ascorbylphosphat und/oder Ascorbylglucosid und/oder Ascorbyltetraisopalmitat enthalten.Preference is given to cosmetic or dermatological compositions according to the invention which contain ascorbyl phosphate and / or ascorbyl glucoside and / or ascorbyl tetraisopalmitate.

Abgesehen von der Ascorbinsäure und/oder Ascorbinsäuresalzen und/oder Ascorbinsäurederivaten können die erfindungsgemäßen Mittel in einer weiteren bevorzugten Ausführungsform weiterhin wenigstens einen pflegenden Wirkstoff, ausgewählt aus der Gruppe der Vitamine, Provitamine oder Vitaminvorstufen, enthalten. Diese sind in den erfindungsgemäßen Mitteln in einer Menge von 0,1 - 10 Gew.-%, vorzugsweise 0,2 - 5 Gew.-% und insbesondere 0,5 - 1 Gew.-%, jeweils bezogen auf das Gesamtgewicht der Mittel, enthalten. Dabei sind erfindungsgemäß solche Vitamine, Pro-Vitamine und Vitaminvorstufen bevorzugt, die üblicherweise den Gruppen A, B, F und H zugeordnet werden.Apart from the ascorbic acid and / or ascorbic acid salts and / or ascorbic acid derivatives, in a further preferred embodiment the compositions according to the invention may further comprise at least one conditioning agent selected from the group of vitamins, provitamins or vitamin precursors. These are in the inventive compositions in an amount of 0.1 to 10 wt .-%, preferably 0.2 to 5 wt .-% and in particular 0.5 to 1 wt .-%, each based on the total weight of the funds, contain. According to the invention, such vitamins, pro-vitamins and vitamin precursors are preferred, which are usually assigned to groups A, B, F and H.

Zur Gruppe der als Vitamin A bezeichneten Substanzen gehören das Retinol (Vitamin A1) sowie das 3,4-Didehydroretinol (Vitamin A2). Das β-Carotin ist das Provitamin des Retinols. Als Vitamin A-Komponente kommen erfindungsgemäß beispielsweise Vitamin A-Säure und deren Ester, Vitamin A-Aldehyd und Vitamin A-Alkohol sowie dessen Ester wie das Palmitat und das Acetat in Betracht.The group of substances called vitamin A includes retinol (vitamin A1) and 3,4-didehydroretinol (vitamin A2). The β-carotene is the provitamin of retinol. As vitamin A component according to the invention, for example, vitamin A acid and its esters, vitamin A aldehyde and vitamin A alcohol and its esters such as the palmitate and the acetate into consideration.

Zur Vitamin B-Gruppe oder Vitamin B-Komplex gehören u. a.

  • Vitamin B1 (Thiamin)
  • Vitamin B2 (Riboflavin)
  • Vitamin B3. Unter dieser Bezeichnung werden häufig die Verbindungen Nicotinsäure und Nicotinsäureamid (Niacinamid) geführt, unter denen insbesondere das Nicotinsäureamid erfindungsgemäß bevorzugt ist.
  • Vitamin B5 (Pantothensäure und Panthenol). Im Rahmen dieser Gruppe wird bevorzugt das Panthenol eingesetzt. Erfindungsgemäß einsetzbare Derivate des Panthenols sind insbesondere die Ester und Ether des Panthenols, kationisch derivatisierte Panthenole sowie Pantolacton.
  • Vitamin B6 (Pyridoxin sowie Pyridoxamin und Pyridoxal).
The vitamin B group or vitamin B complex includes, among others
  • Vitamin B1 (thiamine)
  • Vitamin B2 (riboflavin)
  • Vitamin B3. Under this name, the compounds nicotinic acid and nicotinamide (niacinamide) are often performed, among which in particular the nicotinic acid amide is preferred according to the invention.
  • Vitamin B5 (pantothenic acid and panthenol). Within this group the panthenol is preferred. Derivatives of panthenol which can be used according to the invention are, in particular, the esters and ethers of panthenol, cationically derivatized panthenols and pantolactone.
  • Vitamin B6 (pyridoxine and pyridoxamine and pyridoxal).

Unter dem Begriff "Vitamin F" werden üblicherweise essentielle Fettsäuren, insbesondere Linolsäure, Linolensäure und Arachidonsäure, verstanden.The term "vitamin F" is usually understood as meaning essential fatty acids, in particular linoleic acid, linolenic acid and arachidonic acid.

Als Vitamin H wird die Verbindung (3aS, 4S, 6aR)-2-Oxohexahydrothienol[3,4-d]-imidazol-4-valeriansäure bezeichnet, für die sich aber zwischenzeitlich der Trivialname Biotin durchgesetzt hat.Vitamin H is the compound (3aS, 4S, 6aR) -2-oxohexahydrothienol [3,4-d] -imidazole-4-valeric acid, for which, however, the trivial name biotin has meanwhile prevailed.

Es ist auch vorteilhaft im Sinne der vorliegenden Erfindung, kosmetische oder dermatologische Mittel zu erstellen, deren hauptsächlicher Zweck nicht der Schutz vor Sonnenlicht ist, die aber dennoch einen Gehalt an weiteren UV-Schutzsubstanzen enthalten.It is also advantageous in the context of the present invention to prepare cosmetic or dermatological agents whose main purpose is not the protection from sunlight, but which nevertheless contain a content of further UV protective substances.

Die erfindungsgemäß zu verwendenden UV-Filter unterliegen hinsichtlich ihrer Struktur und ihrer physikalischen Eigenschaften keinen generellen Einschränkungen. Vielmehr eignen sich alle im Kosmetikbereich einsetzbaren UV-Filter, deren Absorptionsmaximum im UVA(315-400 nm)-, im UVB(280-315nm)- oder im UVC(<280 nm)-Bereich liegt. Die UVA-, UVB- und UVC-Filter können sowohl einzeln als auch in Mischungen eingesetzt werden. UV-Filter mit einem Absorptionsmaximum im UVB-Bereich, insbesondere im Bereich von etwa 280 bis etwa 300 nm, sind besonders bevorzugt.The UV filters to be used according to the invention are not subject to any general restrictions with regard to their structure and their physical properties. On the contrary, all UV filters which can be used in the cosmetics sector and whose absorption maximum lies in the UVA (315-400 nm), in the UVB (280-315 nm) or in the UVC (<280 nm) range are suitable. The UVA, UVB and UVC filters can be used individually or in mixtures. UV filters with an absorption maximum in the UVB range, in particular in the range from about 280 to about 300 nm, are particularly preferred.

Der Einsatz von mindestens einer anorganischen und/oder mindestens einer organischen UV-Filtersubstanz ist erfindungsgemäß bevorzugt.The use of at least one inorganic and / or at least one organic UV filter substance is preferred according to the invention.

Die erfindungsgemäß bevorzugten organischen UV-Filter sind ausgewählt aus den Derivaten von Dibenzoylmethan, Zimtsäureestern, Diphenylacrylsäureestern, Benzophenon, Campher, p-Aminobenzoesäureestern, o-Aminobenzoesäureestern, Salicylsäureestern, Benzimidazolen, symmetrisch oder unsymmetrisch substituierten 1,3,5-Triazinen, monomeren und oligomeren 4,4-Diarylbutadiencarbonsäureestern und -carbonsäureamiden, Ketotricyclo(5.2.1.0)decan, Benzalmalonsäureestern, Benzoxazol sowie beliebigen Mischungen der genannten Komponenten. Die organischen UV-Filter können öllöslich oder wasserlöslich sein. Die Benzoxazol-Derivate liegen vorteilhaft in gelöster Form in den erfindungsgemäßen kosmetischen Zubereitungen vor. Es kann ggf. aber auch von Vorteil sein, wenn die Benzoxazol-Derivate in pigmentärer, d. h. ungelöster Form - beispielsweise in Partikelgrößen von 10 nm bis zu 300 nm - vorliegen. Erfindungsgemäß besonders bevorzugte öllösliche UV-Filter sind 1-(4-tert.-Butylphenyl)-3-(4'-methoxyphenyl)propan-1,3-dion (Parsol® 1789), 1-Phenyl-3-(4'-isopropylphenyl)-propan-1,3-dion, 3-(4'-Methylbenzyliden)-D,L-campher, 4-(Dimethylamino)-benzoesäure-2-ethylhexylester, 4-(Dimethylamino)benzoesäure-2-octylester, 4-(Dimethylamino)-benzoesäureamylester, 4-Methoxyzimtsäure-2-ethylhexylester, 4-Methoxyzimt-säurepropylester, 4-Methoxyzimtsäureisopentylester, 2-Cyano-3,3-phenylzimtsäure-2-ethyl-hexylester (Octocrylene), Salicylsäure-2-ethylhexylester, Salicylsäure-4-isopropylbenzylester, Salicylsäurehomomenthylester (3,3,5-Trimethyl-cyclohexylsalicylat), 2-Hydroxy-4-methoxyben-zophenon, 2-Hydroxy-4-methoxy-4'-methylbenzophenon, 2,2'-Dihydroxy-4-methoxybenzophenon, 2-(4'-Diethylamino-2'-hydroxybenzoyl)-benzoesäurehexylester (auch: Aminobenzophenon, unter der Bezeichnung Uvinul A Plus bei der Firma BASF erhältlich), 4-Methoxybenzmalonsäuredi-2-ethylhexylester, an Polymere gebundene UV-Filter, z. B. das 3-(4-(2,2-Bis-Ethoxycarbonylvinyl)-phenoxy)propenyl)-methoxysiloxan/Dimethylsiloxan-Copolymer mit der INCI-Bezeichnung Dimethicodiethylbenzal malonate (CAS-Nr. 207574-74-1, Parsol® SLX), Triazinderivate, wie z. B. 2,4-Bis-{[4-(2-Ethyl-hexyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1,3,5-triazin (INCI: Bis-Ethylhexyloxyphenol Methoxyphenyl Triazin, unter dem Namen Tinosorb S bei CIBA erhältlich), Dioctylbutylamidotriazon (INCI: Diethylhexyl Butamido Triazone, unter dem Namen Uvasorb® HEB bei Sigma 3V erhältlich), 2,4,6-Trianilino-(p-carbo-2'-ethyl-1'-hexyloxy)-1,3,5-triazin (Ethylhexyl Triazone, Uvinul® T 150), 2-[4,6-Bis(2,4-dimethylphenyl)-1,3,5-triazin-2-yl]-5-(octyloxy)phenol (CAS Nr.: 2725-22-6), 2,4-bis-[5-1(di-methylpropyl)benzoxazol-2-yl-(4-phenyl)-imino]-6-(2-ethylhexyl)-imino-1,3,5-triazin (CAS Nr. 288254-16-0, Uvasorb® K2A von 3V Sigma), die Benzotriazolderivate 2,2'-Methylen-bis-(6-(2H-benzotriazol-2-yl)-4-(1,1,3,3-tetramethylbutyl)-phenol) [Tinosorb M (Ciba)], 2,2'-Methyl-bis-[6(2H-benzotriazol-2-yl)-4-(methyl)phenol] (MIXXIM BB/200 der Firma Fairmount Chemical), 2-(2'-Hydroxy-3',5'-di-t-amylphenyl)benzotriazol (CAS- Nr.: 025973-551), 2-(2'-Hydroxy-5'-octylphenyl)-benzotriazol (CAS-Nr. 003147-75-9), 2-(2'-Hydroxy-5'-methylphenyl)benzotriazol (CAS-Nr. 2440-22-4), 2-(2H-benzotriazol-2-yl)-4-methyl-6-[2-methyl-3-[1,3,3,3-tetramethyl-1-((tri-methylsilyl)oxy]disiloxanyl)propyl]-phenol (CAS-Nr.: 155633-54-8) mit der INCI-Bezeichnung Drometrizole Trisiloxane, 2,4-Bis-{[4-(2-ethyl-hexyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1,3,5-triazin (INCI: Bis-Ethylhexyloxyphenol Methoxyphenyl Triazin oder auch Aniso Triazin, erhältlich als Tinosorb® S von CIBA), 2,4-Bis-{[4-(3-sulfonato)-2-hydroxy-propyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1,3,5-triazin-Natriumsalz, 2,4-Bis-{[4-(3-(2-propyloxy)-2-hydroxy-propyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1,3,5-triazin, 2,4-Bis-{[4-(2-ethyl-hexyloxy)-2-hydroxy]-phe-nyl}-6-[4-(2-methoxyethylcarboxyl)-phenylamino]-1,3,5-triazin, 2,4-Bis-{[4-(3-(2-propyloxy)-2-hydro-xy-propyloxy)-2-hydroxy]-phenyl}-6-[4-(ethylcarboxyl)-phenylamino]-1,3,5-triazin, 2,4-Bis-{[4-(2-ethylhexyloxy)-2-hydroxy]-phenyl}-6-(1-methyl-pyrrol-2-yl)-1,3,5-triazin, 2,4-Bis-{[4-tris(trimethylsil-oxy-silylpropyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1,3,5-triazin, 2,4-Bis-{[4-(2-methylpro-penyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1,3,5-triazin, 2,4-Bis-{[4-(1',1',1',3',5',5',5'-Heptamethylsiloxy-2-methyl-propyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1,3,5-triazin sowie Mischungen der genannten Komponenten.The organic UV filters preferred according to the invention are selected from the derivatives of dibenzoylmethane, cinnamic acid esters, diphenylacrylic esters, benzophenone, camphor, p-aminobenzoic acid esters, o-aminobenzoic acid esters, salicylic acid esters, benzimidazoles, symmetrically or unsymmetrically substituted 1,3,5-triazines, monomeric and oligomeric 4,4-Diarylbutadienecarboxylic acid esters and carboxamides, ketotricyclo (5.2.1.0) decane, benzalmalonic acid esters, Benzoxazole and any mixtures of the components mentioned. The organic UV filters can be oil-soluble or water-soluble. The benzoxazole derivatives are advantageously present in dissolved form in the cosmetic preparations according to the invention. However, it may also be advantageous if the benzoxazole derivatives are present in a pigmentary, ie undissolved form, for example in particle sizes of from 10 nm to 300 nm. According to the invention particularly preferred oil-soluble UV filters are 1- (4-tert-butylphenyl) -3- (4'-methoxyphenyl) propane-1,3-dione (Parsol ® 1789), 1-phenyl-3- (4'- isopropylphenyl) -propane-1,3-dione, 3- (4'-methylbenzylidene) -D, L-camphor, 4- (dimethylamino) benzoic acid 2-ethylhexyl ester, 4- (dimethylamino) benzoic acid 2-octyl ester, 4 - (dimethylamino) benzoic acid ester, 4-methoxycinnamic acid 2-ethylhexyl ester, 4-methoxycinnamic acid propyl ester, 4-methoxycinnamic acid isopentyl ester, 2-cyano-3,3-phenylcinnamic acid 2-ethylhexyl ester (octocrylene), salicylic acid 2-ethylhexylester, Salicylic acid 4-isopropylbenzyl ester, salicylic acid homomenthyl ester (3,3,5-trimethylcyclohexylsalicylate), 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxy-4'-methylbenzophenone, 2,2'-dihydroxy-4 -methoxybenzophenone, 2- (4'-diethylamino-2'-hydroxybenzoyl) -benzoesäurhexylester (also: aminobenzophenone, available under the name Uvinul A Plus from BASF), 4-Methoxybenzmalonsäuredi-2-ethylhexyl ester, of polymers bound UV filters, eg. B. 3- (4- (2,2-bis-ethoxycarbonylvinyl) phenoxy) propenyl) -methoxysiloxan / dimethylsiloxane copolymer with the INCI name Dimethicodiethylbenzal malonate (CAS no. 207574-74-1, Parsol ® SLX) , Triazine derivatives, such as. For example, 2,4-bis - {[4- (2-ethyl-hexyloxy) -2-hydroxy] -phenyl} -6- (4-methoxyphenyl) -1,3,5-triazine (INCI: bis-ethylhexyloxyphenol methoxyphenyl triazine, available under the name Tinosorb S from CIBA), dioctylbutylamidotriazone (INCI: Diethylhexyl Butamido Triazone, available under the name Uvasorb HEB from Sigma 3V ®), 2,4,6-trianilino- (p-carbo-2'-ethyl- 1'-hexyloxy) -1,3,5-triazine (ethylhexyl triazone, Uvinul ® T 150), 2- [4,6-bis (2,4-dimethylphenyl) -1,3,5-triazin-2-yl ] -5- (octyloxy) phenol (CAS No .: 2725-22-6), 2,4-bis [5-1 (di-methylpropyl) benzoxazol-2-yl (4-phenyl) -imino] - 6- (2-ethylhexyl) imino-1,3,5-triazine (CAS no. 288254-16-0, Uvasorb K2A ® from 3V Sigma), the benzotriazole derivatives of 2,2'-methylene-bis- (6- ( 2H-benzotriazol-2-yl) -4- (1,1,3,3-tetramethylbutyl) -phenol) [Tinosorb M (Ciba)], 2,2'-methyl-bis- [6 (2H-benzotriazole-2 -yl) -4- (methyl) phenol] (MIXXIM BB / 200 from Fairmount Chemical), 2- (2'-hydroxy-3 ', 5'-di-t-amylphenyl) benzotriazole (CAS No .: 025973 -551), 2- (2'-hydroxy-5'-octylphenyl) benzot riazole (CAS no. 003147-75-9), 2- (2'-hydroxy-5'-methylphenyl) benzotriazole (CAS No. 2440-22-4), 2- (2H-benzotriazol-2-yl) -4-methyl-6 - [2-methyl-3- [1,3,3,3-tetramethyl-1 - ((tri-methylsilyl) oxy] disiloxanyl) propyl] -phenol (CAS No .: 155633-54-8) with the INCI -Credication Drometrizole Trisiloxanes, 2,4-bis - {[4- (2-ethyl-hexyloxy) -2-hydroxy] -phenyl} -6- (4-methoxyphenyl) -1,3,5-triazine (INCI: Bis -Ethylhexyloxyphenol methoxyphenyl triazine or Aniso triazine, available as Tinosorb S from CIBA ®), 2,4-bis - {[4- (3-sulfonato) -2-hydroxy-propyloxy) -2-hydroxy] phenyl} -6 - (4-methoxyphenyl) -1,3,5-triazine sodium salt, 2,4-bis - {[4- (3- (2-propyloxy) -2-hydroxy-propyloxy) -2-hydroxy] -phenyl} -6- (4-methoxyphenyl) -1,3,5-triazine, 2,4-bis - {[4- (2-ethyl-hexyloxy) -2-hydroxy] -phenyl} -6- [4- (2-methoxyethylcarboxyl) phenylamino] -1,3,5-triazine, 2,4-bis - {[4- (3- (2-propyloxy) -2-hydroxy-propyloxy) -2-hydroxy] - phenyl} -6- [4- (ethylcarboxyl) -phenylamino] -1,3,5-triazine, 2,4-bis - {[4- (2-ethylhexyloxy) -2-hydroxy] -phenyl} -6- ( 1-methyl-pyrrol-2-yl) -1,3,5 triazine, 2,4-bis - {[4-tris (trimethylsil-oxy-silylpropyloxy) -2-hydroxy] -phenyl} -6- (4-methoxyphenyl) -1,3,5-triazine, 2,4-bis { [4- (2-methylpropenyloxy) -2-hydroxy] -phenyl} -6- (4-methoxyphenyl) -1,3,5-triazine, 2,4-bis - [[4- (1 ', 1 ', 1', 3 ', 5', 5 ', 5'-Heptamethylsiloxy-2-methyl-propyloxy) -2-hydroxy] -phenyl} -6- (4-methoxyphenyl) -1,3,5-triazine and Mixtures of the components mentioned.

Bevorzugte wasserlösliche UV-Filter sind 2-Phenylbenzimidazol-5-sulfonsäure, Phenylen-1,4-bis-(2-benzimidazyl)-3,3'-5,5'-tetrasulfonsäure und deren Alkali-, Erdalkali-, Ammonium-, Alkylammonium-, Alkanolammonium- und Glucammoniumsalze, insbesondere die Sulfonsäure selbst mit der INCI-Bezeichnung Phenylbenzimidazole Sulfonic Acid (CAS.-Nr. 27503-81-7), die beispielsweise unter dem Handelsnamen Eusolex 232 bei Merck oder unter Neo Heliopan Hydro bei Symrise erhältlich ist, und das Phenylen-1,4-bis-(2-benzimidazyl)-3,3'-5,5'-tetrasulfonsäure-bis-natriumsalz mit der INCI-Bezeichnung Disodium Phenyl Dibenzimidazol Tetrasulfonate (CAS-Nr.: 180898-37-7), das beispielsweise unter dem Handelsnamen Neo Heliopan AP bei Symrise erhältlich ist, Sulfonsäurederivate von Benzophenonen, vorzugsweise 2-Hydroxy-4-methoxybenzophenon-5-sulfonsäure und ihre Salze, Sulfonsäurederivate des 3-Benzylidencamphers, wie z. B. 4-(2-Oxo-3-bornylidenmethyl)benzolsulfonsäure und 2-Methyl-5-(2-oxo-3-bornyliden)sulfonsäure und deren Salze mit der INCI-Bezeichnung Terephthalydene Dicampher Sulfonic Acid (CAS.-Nr.: 90457-82-2, als Mexoryl SX von der Firma Chimex erhältlich).Preferred water-soluble UV filters are 2-phenylbenzimidazole-5-sulfonic acid, phenylene-1,4-bis (2-benzimidazyl) -3,3'-5,5'-tetrasulfonic acid and their alkali metal, alkaline earth metal, ammonium, Alkylammonium, Alkanolammonium- and Glucammoniumsalze, in particular the sulfonic acid itself with the INCI name Phenylbenzimidazole Sulfonic Acid (CAS No. 27503-81-7), for example, under the trade name Eusolex 232 at Merck or Neo Heliopan Hydro available from Symrise and the phenylene-1,4-bis (2-benzimidazyl) -3,3'-5,5'-tetrasulfonic acid bis-sodium salt with the INCI name Disodium Phenyl Dibenzimidazole Tetrasulfonate (CAS No .: 180898- 37-7), which is available for example under the trade name Neo Heliopan AP Symrise, sulfonic acid derivatives of benzophenones, preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and its salts, sulfonic acid derivatives of 3-Benzylidencamphers such. B. 4- (2-oxo-3-bionylidenemethyl) benzenesulfonic acid and 2-methyl-5- (2-oxo-3-bomylidene) sulfonic acid and its salts with the INCI name Terephthalydene Dicampher Sulfonic Acid (CAS. 90457-82-2, available as Mexoryl SX from Chimex).

Auch anorganische Pigmente können erfindungsgemäß als UV-Filter eingesetzt werden. Bevorzugte anorganische Pigmente sind Metalloxide und/oder andere in Wasser schwerlösliche oder unlösliche Metallverbindungen, beispielsweise Carbonate, Sulfate usw. Bevorzugt sind insbesondere Oxide des Titans (TiO2), Zinks (ZnO), Eisens (z. B. Fe 2O3), Zirkoniums (ZrO2), Siliciums (SiO 2), Mangans (z. B. MnO), Aluminiums (Al2O3), Cers (z. B. Ce2O3), Mischoxide der entsprechenden Metalle sowie Abmischungen aus solchen Oxiden sowie das Sulfat des Bariums (BaSO4).Inorganic pigments can also be used according to the invention as UV filters. Preferred inorganic pigments are metal oxides and / or other sparingly water-soluble or insoluble metal compounds, for example carbonates, sulfates, etc. Preferred oxides of titanium (TiO 2), zinc (ZnO), iron (eg Fe 2 O 3), zirconium (ZrO 2 ), Silicon (SiO 2), manganese (eg MnO), aluminum (Al 2 O 3), cerium (eg Ce 2 O 3), mixed oxides of the corresponding metals as well as mixtures of such oxides and the barium sulfate (BaSO 4).

Die anorganischen Pigmente können einen mittleren Teilchendurchmesser von maximal 200 µm haben und aus den Oxiden von Silicium, Titan, Eisen, Zink, Zirkonium, Magnesium, Cer und Bismut, aus Bornitrid, Glimmer, Flussspat und wasserunlöslichen Perlglanzpigmenten, die mit mindestens einer anorganischen und/oder organischen Verbindung beschichtet sein können, ausgewählt sein. Bevorzugte anorganische Pigmente weisen einen Durchmesser von 1 bis 100 µm auf, besonders bevorzugt 1 bis 50 µm, und außerordentlich bevorzugt 1 bis 10 µm.The inorganic pigments may have a maximum average particle diameter of 200 microns and from the oxides of silicon, titanium, iron, zinc, zirconium, magnesium, cerium and bismuth, boron nitride, mica, fluorspar and water-insoluble pearlescent pigments containing at least one inorganic and / or or organic compound may be selected. Preferred inorganic pigments have a diameter of 1 to 100 .mu.m, more preferably 1 to 50 .mu.m, and most preferably 1 to 10 .mu.m.

Die Pigmente können sowohl farbig als auch farblos sein. Die bevorzugten Pigmente sind ausgewählt aus den Oxiden von Silicium, Titan, Zink und Eisen, sowie aus Bismutoxychlorid. Weitere erfindungsgemäß bevorzugte Pigmente sind Glimmer und Perlglanzpigmente.The pigments can be both colored and colorless. The preferred pigments are selected from the oxides of silicon, titanium, zinc and iron, as well as bismuth oxychloride. Further preferred pigments according to the invention are mica and pearlescent pigments.

Die genannten anorganischen Pigmente können beschichtet sein. Die Beschichtung kann mit Hilfe von anorganischen und/oder organischen Verbindungen erfolgen. Erfindungsgemäß bevorzugt sind anorganische Pigmente, die eine anorganische Beschichtung aufweisen.The said inorganic pigments may be coated. The coating can be carried out with the aid of inorganic and / or organic compounds. According to the invention, preference is given to inorganic pigments which have an inorganic coating.

Bevorzugte Pigmente dieser Art sind ausgewählt aus Siliciumdioxid-Partikeln, die mit Titandioxid und/oder Eisenoxiden beschichtet sind. Ein besonders bevorzugtes Pigment dieser Art ist das Handelsprodukt Ronasphere®LDP der Firma Merck KGaA. Bei diesem Produkt handelt es sich um sphärische Siliciumdioxid-Partikel, die mit Titandioxid und Eisenoxid beschichtet sind. Ronasphere®LDP weist einen Brechungsindex auf, der dem Brechungsindex der Haut ähnelt.Preferred pigments of this type are selected from silica particles coated with titanium dioxide and / or iron oxides. A particularly preferred pigment of this type is the commercial product Ronasphere® LDP from Merck KGaA. This product is a spherical silica particle coated with titanium dioxide and iron oxide. Ronasphere® LDP has a refractive index that is similar to the refractive index of the skin.

Weiterhin geeignet sind anorganisch beschichtete Glimmerpigmente, die keinen Perlglanz aufweisen.Also suitable are inorganic-coated mica pigments which have no pearlescence.

Weitere bevorzugte anorganisch beschichtete anorganische Pigmente sind Glimmerpigmente, die mit Titandioxid in verschiedenen Schichtdicken beschichtet sind, beispielsweise das Produkt RonaFlair® Extender W von Merk KGaA. Das genannte Produkt wies durchschnittliche Teilchendurchmesser von 3 - 8 µm auf. Ebenfalls bevorzugt sind Glimmerpartikel mit einer Beschichtung aus Metalloxidmischung. Weitere erfindungsgemäß geeignete Pigmente sind anorganisch beschichtete anorganische Pigmente, deren Beschichtung einen Anteil von 0,1 - 5 Gew.-% Zinnoxid aufweist.Further preferred inorganic-coated inorganic pigments are mica pigments which are coated with titanium dioxide in various layer thicknesses, for example the product RonaFlair® Extender W from Merk KGaA. The named product had average particle diameters of 3 to 8 μm. Also preferred are mica particles having a coating of metal oxide mixture. Other pigments which are suitable according to the invention are inorganic-coated inorganic pigments whose coating has a proportion of 0.1-5% by weight of tin oxide.

Ebenfalls erfindungsgemäß geeignet, wenngleich weniger bevorzugt, sind anorganische Pigmente, die mit organischen Substanzen beschichtet sind. Beispiele hierfür sind mit Aluminiumstearat beschichtete Titandioxid-Pigmente, mit Dimethylpolysiloxan (Dimethicone) beschichtetes Zinkoxid, mit Dimethicone beschichtetes Bornitrid, mit einem Gemisch aus Dimethylpolysiloxan und Silicagel (Simethicone) und Aluminiumoxidhydrat (Alumina) beschichtetes Titandioxid, mit Octylsilanol beschichtetes Titandioxid oder sphärische Polyalkylsesquisiloxan-Partikel.Also suitable according to the invention, although less preferred, are inorganic pigments coated with organic substances. Examples include aluminum stearate coated titanium dioxide pigments, dimethylpolysiloxane (dimethicone) coated zinc oxide, dimethicone coated boron nitride, a mixture of dimethylpolysiloxane and silica gel (simethicone) and alumina hydrate (alumina) coated titania, octylsilanol coated titania or spherical polyalkylsesquisiloxane particles ,

In einer bevorzugten Ausführungsform enthalten die erfindungsgemäßen Mittel mindestens ein Metalloxid, vorzugsweise ein Metalloxid als hautaufhellenden Wirkstoff. Hier sind erfindungsgemäße kosmetische oder dermatologische Mittel bevorzugt, die bezogen auf ihr Gesamtgewicht, insgesamt 0,01 bis 5 Gew.-%, vorzugsweise 0,1 bis 3 Gew.-% Metalloxid, bevorzugt Metalloxid als hautaufhellenden Wirkstoff enthalten. Erfindungsgemäß vorzugsweise einsetzbar ist Titandioxid.In a preferred embodiment, the agents according to the invention comprise at least one metal oxide, preferably a metal oxide as skin-lightening active ingredient. Here, cosmetic or dermatological agents according to the invention are preferred which contain, based on their total weight, a total of 0.01 to 5 wt .-%, preferably 0.1 to 3 wt .-% metal oxide, preferably metal oxide as skin-lightening agent. Titanium dioxide is preferably usable according to the invention.

Die erfindungsgemäßen Mittel enthalten die jeweiligen Wirkstoffe in einem kosmetisch verträglichen Träger. Dieser kosmetische Träger ist bevorzugt wässrig, alkoholisch, wässrigalkoholisch oder wässrig-glycolisch. Solche Träger sind beispielsweise Cremes, Emulsionen, Gele oder auch tensidhaltige schäumende Lösungen, wie beispielsweise Duschgele oder andere Zubereitungen, die für die Anwendung auf der Haut geeignet sind. Ein wässriger Träger enthält im Sinne der Erfindung bevorzugt mindestens 40 Gew.-%, besonders bevorzugt mindestens 50 Gew.-% Wasser. Erfindungsgemäß bevorzugte kosmetische Mittel sind dadurch gekennzeichnet, daß sie, bezogen auf das Gesamtgewicht des anwendungsbereiten Mittels 10 bis 80 Gew.-%, vorzugsweise 20 bis 75 Gew.-%, weiter bevorzugt 30 bis 70 Gew.-%, noch weiter bevorzugt 35 bis 60 Gew.-% und insbesondere 40 bis 60 Gew.-% Wasser enthalten.The compositions of the invention contain the respective active ingredients in a cosmetically acceptable carrier. This cosmetic carrier is preferably aqueous, alcoholic, aqueous-alcoholic or aqueous-glycolic. Such carriers are, for example, creams, emulsions, gels or surfactant-containing foaming solutions, such as shower gels or other preparations which are suitable for use on the skin. An aqueous carrier contains in According to the invention preferably at least 40 wt .-%, particularly preferably at least 50 wt .-% water. Cosmetic agents preferred according to the invention are characterized in that they contain 10 to 80% by weight, preferably 20 to 75% by weight, more preferably 30 to 70% by weight, even more preferably 35 to 100% by weight, based on the total weight of the ready-to-use agent 60 wt .-% and in particular 40 to 60 wt .-% water.

Unter wässrig-alkoholischen Trägern sind im Sinne der vorliegenden Erfindung wasserhaltige Zusammensetzungen, enthaltend 3 bis 70 Gew.-%, bevorzugt 10 - 60 Gew.-%, besonders bevorzugt 15 - 40 Gew.-%, eines einwertigen C2-C4-Alkohols, insbesondere Ethanol, zu verstehen.In the context of the present invention, aqueous-alcoholic carriers are water-containing compositions containing from 3 to 70% by weight, preferably from 10 to 60% by weight, particularly preferably from 15 to 40% by weight, of a monohydric C 2 -C 4 -alcohol. especially ethanol, to understand.

Unter wässrig-glycolischen Trägern sind im Sinne der vorliegenden Erfindung wasserhaltige Zusammensetzungen, enthaltend 3 bis 70 Gew.-%, bevorzugt 10 - 60 Gew.-%, besonders bevorzugt 15 - 40 Gew.-%, mindestens eines zwei- oder mehrwertigen C2-C9-Alkohols oder mindestens eines wasserlöslichen Polyethylenglycols mit 3 - 20 Ethylenoxid-Einheiten, insbesondere ausgewählt aus 1,2-Propylenglycol, 2-Methyl-1,3-propandiol, Glycerin, 1,2-Butylenglycol, 1,3-Butylengly-col, 1,4-Butylenglycol, Pentylenglycolen wie 1,2-Pentandiol und 1,5-Pentandiol, Hexandiolen wie 1,6-Hexandiol, Hexantriolen wie 1,2,6-Hexantriol, 1,2-Octandiol, 1,8-Octandiol, Dipropylenglycol, Tripropylenglycol, Diglycerin, Triglycerin, PEG-3, PEG-4, PEG-6, PEG-7, PEG-8, PEG-9, PEG-10, PEG-12, PEG-14, PEG-16, PEG-18 und PEG-20 sowie Mischungen hiervon, zu verstehen.For the purposes of the present invention, aqueous-glycolic carriers are water-containing compositions containing from 3 to 70% by weight, preferably from 10 to 60% by weight, particularly preferably from 15 to 40% by weight, of at least one bivalent or polyvalent C 2 C9 alcohol or at least one water-soluble polyethylene glycol having 3 to 20 ethylene oxide units, in particular selected from 1,2-propylene glycol, 2-methyl-1,3-propanediol, glycerol, 1,2-butylene glycol, 1,3-butylene glycol , 1,4-butylene glycol, pentylene glycols such as 1,2-pentanediol and 1,5-pentanediol, hexanediols such as 1,6-hexanediol, hexanetriols such as 1,2,6-hexanetriol, 1,2-octanediol, 1,8-octanediol , Dipropylene glycol, tripropylene glycol, diglycerol, triglycerol, PEG-3, PEG-4, PEG-6, PEG-7, PEG-8, PEG-9, PEG-10, PEG-12, PEG-14, PEG-16, PEG -18 and PEG-20 and mixtures thereof.

Die erfindungsgemäßen Mittel können zusätzlich weitere organische Lösemittel, wie beispielsweise Methoxybutanol, Ethyldiglycol, 1,2-Propylenglycol, 2-Methyl-1,3-propandiol, n-Propanol, n-Butanol, n-Butylenglycol, Glycerin, Diethylenglycolmonoethylether und Diethylenglycolmono-n-butylether, enthalten. Bevorzugt sind dabei alle wasserlöslichen organischen Lösemittel.The compositions of the invention may additionally contain other organic solvents such as, for example, methoxybutanol, ethyl diglycol, 1,2-propylene glycol, 2-methyl-1,3-propanediol, n-propanol, n-butanol, n-butylene glycol, glycerol, diethylene glycol monoethyl ether and diethylene glycol mono-n butyl ether. Preference is given to all water-soluble organic solvents.

Die erfindungsgemäßen Mittel können in allen für die topische Applikation auf die Haut geeigneten Darreichungsformen konfektioniert sein. Bevorzugte Darreichungsformen sind eine Lösung, eine Emulsion vom Typ Wasser-in-Öl (W/O), eine Emulsion vom Typ Öl-in-Wasser (O/W), eine multiple Emulsion, beispielsweise vom Typ Wasser-in-Öl-in-Wasser (W/O/W) oder Öl-in-Wasser-in-Öl (O/W/O), eine Hydrodispersion, eine Lipodispersion, ein Gel, ein Hydrodispersionsgel, ein Lipodispersionsgel, ein fester Stift, ein Gelpflaster (Gelpatch), ein Pflaster, ein Kataplasma, Wirkstoff-haltige Liposomen oder ein transdermales therapeutisches System. Niedrig-viskose oder mittelviskose Darreichungsformen können auch in einem treibgasfreien Pump- oder Sprühspender oder zusammen mit einem Treibmittel in einem Aerosolbehälter konfektioniert sein.The compositions according to the invention can be formulated in all dosage forms suitable for topical application to the skin. Preferred dosage forms are a solution, a water-in-oil (W / O) type emulsion, an oil-in-water (O / W) type emulsion, a multiple emulsion, for example, water-in-oil-in type Water (W / O / W) or oil-in-water-in-oil (O / W / O), a hydrodispersion, a lipodispersion, a gel, a hydrodispersion gel, a lipodispersion gel, a solid stick, a gel patch (Gelpatch ), a patch, a cataplasm, drug-containing liposomes or a transdermal therapeutic system. Low-viscous or medium-viscosity dosage forms may also be packaged in a propellant-free pump or spray dispenser or together with a propellant in an aerosol container.

Die anwendungsbereiten erfindungsgemäßen Mittel können weitere Wirk-, Hilfs- und Zusatzstoffe enthalten.The ready-to-use agents according to the invention may contain further active ingredients, auxiliaries and additives.

Beispielsweise hat es sich für die Applikation und den Verbleib des Mittels auf der Haut als vorteilhaft erwiesen, wenn die Mittel mindestens ein Verdickungsmittel enthalten. Bezüglich dieserFor example, it has proved to be advantageous for the application and the whereabouts of the agent on the skin if the agents contain at least one thickener. Regarding this

Verdickungsmittel bestehen keine prinzipiellen Einschränkungen. Es können sowohl organische als auch rein anorganische Verdickungsmittel zum Einsatz kommen. Geeignete Verdickungsmittel sind

  • anionische, synthetische Polymere;
  • kationische, synthetische Polymere;
  • natürlich vorkommende Verdickungsmittel, wie Guargums, Skleroglucangums oder Xanthangums, Gummi arabicum, Ghatti-Gummi, Karaya-Gummi, Tragant-Gummi, Carrageen-Gummi, Agar-Agar, Johannisbrotkernmehl, Pektine, Alginate, Stärke-Fraktionen und Derivate wie Amylose, Amylopektin und Dextrine, sowie Cellulosederivate, wie beispielsweise Methylcellulose, Carboxyalkylcellulosen und Hydroxyalkylcellulosen;
  • nichtionische, vollsynthetische Polymere, wie Polyvinylalkohol oder Polyvinylpyrrolidinon; sowie
  • anorganische Verdickungsmittel, insbesondere Schichtsilikate wie beispielsweise Bentonit, besonders Smektite, wie Montmorillonit oder Hectorit.
Thickeners are not subject to any restrictions. Both organic and purely inorganic thickening agents can be used. Suitable thickeners are
  • anionic, synthetic polymers;
  • cationic synthetic polymers;
  • naturally occurring thickening agents such as guar gums, scleroglucan gums or xanthan gums, gum arabic, ghatti gum, karaya gum, gum tragacanth, carrageenan gum, agar agar, locust bean gum, pectins, alginates, starch fractions and derivatives such as amylose, amylopectin and Dextrins, as well as cellulose derivatives such as methylcellulose, carboxyalkylcelluloses and hydroxyalkylcelluloses;
  • nonionic, fully synthetic polymers, such as polyvinyl alcohol or polyvinylpyrrolidinone; such as
  • inorganic thickeners, in particular phyllosilicates such as bentonite, especially smectites, such as montmorillonite or hectorite.

Vorzugsweise werden die Mittel als fließfähige Zubereitungen bereitgestellt. "Fließfähig" im Sinne der vorliegenden Anmeldung sind dabei Zusammensetzungen, die gießbar sind und Viskositäten von 10 mPa·s bis hin zu 250.000 mPa·s (20 °C) aufweisen können. Die Viskosität kann mit üblichen Standardmethoden (beispielsweise Brookfield-Viskosimeter LVT-II bei 20 U/min und 20°C, Spindel 3) gemessen werden und liegt vorzugsweise im Bereich von 50 bis 50000 mPa·s. Bevorzugte Mittel haben Viskositäten von 1000 bis 30000 mPas, wobei Werte von 5000 bis 20000 mPas besonders bevorzugt sind.Preferably, the agents are provided as flowable preparations. "Flowable" in the context of the present application are compositions which are pourable and may have viscosities of from 10 mPa.s up to 250,000 mPa.s (20 ° C.). The viscosity can be measured by conventional standard methods (for example Brookfield LVT-II viscosimeter at 20 rpm and 20 ° C., spindle 3) and is preferably in the range from 50 to 50 000 mPa · s. Preferred agents have viscosities of from 1000 to 30,000 mPas, with values of from 5,000 to 20,000 mPas being particularly preferred.

Erfindungsgemäße Emulsionen im Sinne der vorliegenden Erfindung, z. B. in Form einer Creme, einer Lotion oder einer kosmetischen Milch, sind vorteilhaft und enthalten z. B. Fette, Öle, Wachse und/oder andere Fettkörper, sowie Wasser und einen oder mehrere Emulgatoren, wie sie üblicherweise für einen solchen Typ der Formulierung verwendet werden.According to the invention emulsions, z. As in the form of a cream, a lotion or a cosmetic milk, are advantageous and contain z. As fats, oils, waxes and / or other fatty substances, and water and one or more emulsifiers, such as are commonly used for such a type of formulation.

In einer weiteren bevorzugten Ausführungsform können die erfindungsgemäßen Mittel Emulgatoren enthalten. Emulgatoren bewirken an der Phasengrenzfläche die Ausbildung von wasser- bzw. ölstabilen Adsorptionsschichten, welche die dispergierten Tröpfchen gegen Koaleszenz schützen und damit die Emulsion stabilisieren. Emulgatoren sind daher wie Tenside aus einem hydrophoben und einem hydrophilen Molekülteil aufgebaut. Hydrophile Emulgatoren bilden bevorzugt O/W - Emulsionen und hydrophobe Emulgatoren bilden bevorzugt W/O - Emulsionen. Unter einer Emulsion ist eine tröpfchenförmige Verteilung (Dispersion) einer Flüssigkeit in einer anderen Flüssigkeit unter Aufwand von Energie zur Schaffung von stabilisierenden Phasengrenzflächen mittels Tensiden zu verstehen. Die Auswahl dieser emulgierenden Tenside oder Emulgatoren richtet sich dabei nach den zu dispergierenden Stoffen und der jeweiligen äußeren Phase sowie der Feinteiligkeit der Emulsion. Erfindungsgemäß verwendbare Emulgatoren sind beispielsweise

  • Anlagerungsprodukte von 4 bis 30 Mol Ethylenoxid und/oder 0 bis 5 Mol Propylenoxid an lineare Fettalkohole mit 8 bis 22 C-Atomen, an Fettsäuren mit 12 bis 22 C-Atomen und an Alkylphenole mit 8 bis 15 C-Atomen in der Alkylgruppe,
  • C12-C22-Fettsäuremono- und -diester von Anlagerungsprodukten von 1 bis 30 Mol Ethylenoxid an Polyole mit 3 bis 6 Kohlenstoffatomen, insbesondere an Glycerin,
  • Ethylenoxid- und Polyglycerin-Anlagerungsprodukte an Methylglucosid-Fettsäureester, Fettsäurealkanolamide und Fettsäureglucamide,
  • C8-C22-Alkylmono- und -oligoglycoside und deren ethoxylierte Analoga, wobei Oligomerisierungsgrade von 1,1 bis 5, insbesondere 1,2 bis 2,0, und Glucose als Zuckerkomponente bevorzugt sind,
  • Gemische aus Alkyl-(oligo)-glucosiden und Fettalkoholen zum Beispiel das im Handel erhältliche Produkt Montanov®68,
  • Anlagerungsprodukte von 5 bis 60 Mol Ethylenoxid an Rizinusöl und gehärtetes Rizinusöl,
  • Partialester von Polyolen mit 3-6 Kohlenstoffatomen mit gesättigten Fettsäuren mit 8 bis 22 C-Atomen,
  • Sterine. Als Sterine wird eine Gruppe von Steroiden verstanden, die am C-Atom 3 des Steroid-Gerüstes eine Hydroxylgruppe tragen und sowohl aus tierischem Gewebe (Zoosterine) wie auch aus pflanzlichen Fetten (Phytosterine) isoliert werden. Beispiele für Zoosterine sind das Cholesterin und das Lanosterin. Beispiele geeigneter Phytosterine sind Ergosterin, Stigmasterin und Sitosterin. Auch aus Pilzen und Hefen werden Sterine, die sogenannten Mykosterine, isoliert.
  • Phospholipide. Hierunter werden vor allem die Glucose-Phospolipide, die z.B. als Lecithine bzw. Phosphatidylcholine aus z.B. Eidotter oder Pflanzensamen (z.B. Sojabohnen) gewonnen werden, verstanden.
  • Fettsäureester von Zuckern und Zuckeralkoholen, wie Sorbit,
  • Polyglycerine und Polyglycerinderivate wie beispielsweise Polyglycerinpoly-12-hydroxystearat (Handelsprodukt Dehymuls® PGPH),
  • Lineare und verzweigte Fettsäuren mit 8 bis 30 C - Atomen und deren Na-, K-, Ammonium-, Ca-, Mg- und Zn - Salze.
In a further preferred embodiment, the agents according to the invention may contain emulsifiers. Emulsifiers effect at the phase interface the formation of water- or oil-stable adsorption layers, which protect the dispersed droplets against coalescence and thus stabilize the emulsion. Emulsifiers are therefore constructed like surfactants from a hydrophobic and a hydrophilic part of the molecule. Hydrophilic emulsifiers preferably form O / W emulsions and hydrophobic emulsifiers preferably form W / O emulsions. An emulsion is to be understood as meaning a droplet-like distribution (dispersion) of a liquid in another liquid under the expense of energy in order to create stabilizing phase interfaces by means of surfactants. The selection of these emulsifying surfactants or emulsifiers depends on the substances to be dispersed and the respective outer phase and the fineness of the emulsion. Emulsifiers which can be used according to the invention are, for example
  • Addition products of 4 to 30 moles of ethylene oxide and / or 0 to 5 moles of propylene oxide to linear fatty alcohols having 8 to 22 carbon atoms, to fatty acids having 12 to 22 carbon atoms and to alkylphenols having 8 to 15 carbon atoms in the alkyl group,
  • C12-C22 fatty acid mono- and diesters of addition products of from 1 to 30 moles of ethylene oxide onto polyols having from 3 to 6 carbon atoms, in particular to glycerol,
  • Ethylene oxide and polyglycerol addition products to methyl glucoside fatty acid esters, fatty acid alkanolamides and fatty acid glucamides,
  • C 8 -C 22 -alkylmono- and -oligoglycosides and their ethoxylated analogues, preference being given to degrees of oligomerization of from 1.1 to 5, in particular from 1.2 to 2.0, and glucose as the sugar component,
  • Mixtures of alkyl (oligo) glucosides and fatty alcohols, for example the commercially available product Montanov®68,
  • Addition products of 5 to 60 moles of ethylene oxide with castor oil and hydrogenated castor oil,
  • Partial esters of polyols having 3-6 carbon atoms with saturated fatty acids having 8 to 22 carbon atoms,
  • Sterols. Sterols are understood to mean a group of steroids which have a hydroxyl group on C-atom 3 of the steroid skeleton and are isolated both from animal tissue (zoosterols) and from vegetable fats (phytosterols). Examples of zoosterols are cholesterol and lanosterol. Examples of suitable phytosterols are ergosterol, stigmasterol and sitosterol. Mushrooms and yeasts are also used to isolate sterols, the so-called mycosterols.
  • Phospholipids. These include, in particular, the glucose phospholipids which are obtained, for example, as lecithins or phosphatidylcholines from, for example, egg yolks or plant seeds (for example soybeans).
  • Fatty acid esters of sugars and sugar alcohols, such as sorbitol,
  • Polyglycerols and polyglycerol derivatives such as polyglycerol poly-12-hydroxystearate (commercial product Dehymuls® PGPH),
  • Linear and branched fatty acids with 8 to 30 C atoms and their Na, K, ammonium, Ca, Mg and Zn salts.

Die erfindungsgemäßen Mittel enthalten die Emulgatoren bevorzugt in Mengen von 0,1 - 30 Gew.-%, insbesondere 3 - 15 Gew.-%, bezogen auf das gesamte Mittel.The agents according to the invention preferably contain the emulsifiers in amounts of from 0.1 to 30% by weight, in particular from 3 to 15% by weight, based on the total agent.

Bevorzugt können die erfindungsgemäßen Mittel mindestens einen nichtionogenen Emulgator mit einem HLB-Wert von 8 bis 18 enthalten. Nichtionogene Emulgatoren mit einem HLB-Wert von 10 - 15 können erfindungsgemäß besonders bevorzugt sein.The agents according to the invention may preferably contain at least one nonionic emulsifier having an HLB value of 8 to 18. Nonionic emulsifiers having an HLB value of 10 to 15 may be particularly preferred according to the invention.

Die erfindungsgemäßen Mittel eignen sich zur Aufhellung der Haut und können dementsprechend eingesetzt werden. Dabei kann die Haut lokal begrenzt (z.B. auf Sommersprossen, Altersflecken oder Fehlpigmentierungen) oder großflächig (zur Hautaufhellung) behandelt werden.The compositions according to the invention are suitable for lightening the skin and can be used accordingly. In this case, the skin can be locally limited (for example freckles, age spots or Fehlpigmentierungen) or large (for skin lightening) to be treated.

Weitere Gegenstände der vorliegenden Erfindung sind daher die nicht-therapeutische, kosmetische Verwendung von erfindungsgemäßen kosmetischen oder dermatologischen Mitteln zur Aufhellung der Hautfarbe, zur Reduzierung der Pigmentierung der Haut, zum Ausgleich des Erscheinungsbildes einer ungleichmäßigen Hautpigmentierung und/oder zur Aufhellung von Altersflecken oder Sommersprossen der Haut.Further objects of the present invention are therefore the non-therapeutic, cosmetic use of cosmetic or dermatological agents according to the invention for lightening the skin color, reducing pigmentation of the skin, balancing the appearance of uneven skin pigmentation and / or lightening age spots or freckles of the skin ,

Ein weiterer Gegenstand der vorliegenden Erfindung ist die nicht-therapeutische, kosmetische Verwendung von erfindungsgemäßen kosmetischen und dermatologischen Mittel zur Behandlung postinflammatorischer Hyperpigmentierung.Another object of the present invention is the non-therapeutic, cosmetic use of cosmetic and dermatological agents according to the invention for the treatment of postinflammatory hyperpigmentation.

Bezüglich bevorzugter Ausführungsformen der erfindungsgemäßen Verwendungen gilt mutatis mutandis das zu den erfindungsgemäßen Mittel Gesagte.With respect to preferred embodiments of the uses according to the invention mutatis mutandis applies to the means of the invention.

Ein weiterer Gegenstand der vorliegenden Erfindung ist ein nicht-therapeutisches, kosmetisches Verfahren zur Aufhellung der Hautfarbe, zur Reduzierung der Pigmentierung der Haut, zum Ausgleich des Erscheinungsbildes einer ungleichmäßigen Hautpigmentierung und/oder zur Aufhellung von Altersflecken oder Sommersprossen der Haut, dadurch gekennzeichnet, dass ein kosmetisches Mittel, enthaltend eine Kombination aus mindestens einem der unter a) und mindestens einem der unter b) aufgeführten Wirkstoffe:

  1. a) Extrakt aus Quassia Amara;
  2. b) gesättigte oder ungesättigte, lineare (C9- bis C18)-Dicarbonsäure, insbesondere 8-Hexadecen-1,16-dicarbonsäure und/oder 7-Tetradecen-1, 14-dicarbonsäure und/oder 9-Octadecen-1,18-dicarbonsäure und/oder 6-Dodecen-1,12-dicarbonsäure und/oder 5-Decen-1,10-dicarbonsäure und/oder Decandisäure (Sebacinsäure) und/oder Nonandisäure (Azelainsäure), ganz besonders bevorzugt 8-Hexadecen-1,16-dicarbonsäure,
auf die Haut aufgetragen wird.Another object of the present invention is a non-therapeutic, cosmetic method for whitening the skin color, to reduce the pigmentation of the skin, to compensate for the appearance of uneven skin pigmentation and / or to lighten age spots or freckles of the skin, characterized in that Cosmetic composition containing a combination of at least one of the active substances listed under a) and at least one of the substances listed under b):
  1. a) Extract from Quassia Amara;
  2. b) saturated or unsaturated, linear (C9 to C18) dicarboxylic acid, in particular 8-hexadecene-1,16-dicarboxylic acid and / or 7-tetradecene-1, 14-dicarboxylic acid and / or 9-octadecene-1,18-dicarboxylic acid and / or 6-dodecene-1,12-dicarboxylic acid and / or 5-decene-1,10-dicarboxylic acid and / or decanedioic acid (sebacic acid) and / or nonanedioic acid (azelaic acid), very particularly preferably 8-hexadecene-1,16- dicarboxylic acid,
is applied to the skin.

Bezüglich bevorzugter Ausführungsformen der erfindungsgemäßen Verfahren gilt mutatis mutandis das zu den erfindungsgemäßen Mittel Gesagte.With respect to preferred embodiments of the method according to the invention mutatis mutandis applies to the means of the invention.

Die folgenden Beispiele erläutern die Erfindung, ohne sie jedoch darauf einzuschränken:The following examples illustrate the invention without, however, limiting it to:

Beispiele:Examples:

Es wurden die folgenden kosmetischen oder dermatologischen Mittel hergestellt, wobei alle Zahlenwerte in den nachfolgenden Beispielen - sofern nicht anders angegeben - der Menge des jeweiligen Wirkstoffs in Gewichtsprozent bezogen auf das Gesamtgewicht des Mittels entsprechen:

Figure imgb0002
Figure imgb0003
Figure imgb0004
Figure imgb0005
Figure imgb0006
Figure imgb0007
The following cosmetic or dermatological agents have been prepared, all numerical values in the following examples, unless otherwise stated, corresponding to the amount of the respective active substance in percent by weight, based on the total weight of the composition:
Figure imgb0002
Figure imgb0003
Figure imgb0004
Figure imgb0005
Figure imgb0006
Figure imgb0007

Die erfindungsgemäßen Mittel nach Formel 66 wurden in einem Gebrauchstest unter dermatologischer Kontrolle an 50 Probandinnen mit Altersflecken im Gesicht geprüft. Die Testpersonen sollten dabei die Mittel über insgesamt 4 Wochen mindestens zweimal täglich zur Gesichtspflege anwenden. Der dermatologische Gebrauchstest der erfindungsgemäßen Mittel im Vergleich zur Mittelvariante, die kein Quassia amara Extrakt enthält, ergibt, dass die erfindungsgemäßen Mittel mit Extrakt aus Quassia amara viel bessere Aufhellungseffekte gegen Hautflecken zeigen und die Haut wirksamer gegen das Auftreten neuer Hautflecken schützten. Verwendete Rohstoffe Handelsname INCI-Bezeichnung Lieferant/ Hersteller Quassia Amara A 00264 Quassia Amara Wood Extract BASF Cetiol® SB 45 Butyrospermum Parkii (Schea Butter) Cognis Cetiol® SN Cetearyl Isononanoate Cognis Cutina MD Glyceryl Stearate Cognis RonaFlair® Extender W MICA, CI 77891 (Titanium Dioxide) Merck RonaFlair® Balance Gold Mica, CI 77891 (Titanium Dioxide), Tin Oxide Merck Montanov 202 Arachidyl Alcohol, Behenyl alcohol, Arachidyl Glucoside Seppic Nikkol VC IP Ascorbyl Tetraisopalmitate Nikko Chemicals Nikkol VC PMG C Magnesium Ascorbyl Phosphate Nikko Chemicals ODA White Octadecenedioic Acid, BHT Croda Uvinul T 150 Ethylhexyl triazone BASF The compositions of the invention according to formula 66 were tested in a use test under dermatological control on 50 subjects with age spots on the face. The test subjects should use the funds for facial care at least twice a day for a total of 4 weeks. The dermatological use test of the compositions according to the invention in comparison to the middle variant which does not contain Quassia amara extract shows that the compositions according to the invention with Quassia amara extract show much better whitening effects against skin spots and protect the skin more effectively against the appearance of new skin patches. Used raw materials trade name INCI name Supplier / Manufacturer Quassia Amara A 00264 Quassia Amara Wood Extract BASF Cetiol ® SB 45 Butyrospermum Parkii (Schea Butter) Cognis Cetiol ® SN Cetearyl Isononanoate Cognis Cutina MD Glyceryl stearate Cognis RonaFlair ® Extender W MICA, CI 77891 (Titanium Dioxide) Merck RonaFlair ® Balance Gold Mica, CI 77891 (Titanium Dioxide), Tin Oxide Merck Montanov 202 Arachidyl alcohol, Behenyl alcohol, Arachidyl glucoside Seppic Nikkol VC IP Ascorbyl tetraisopalmitate Nikko Chemicals Nikkol VC PMG C Magnesium ascorbyl phosphate Nikko Chemicals ODA White Octadecenedioic Acid, BHT Croda Uvinul T 150 Ethylhexyl triazone BASF

Claims (10)

Kosmetisches oder dermatologisches Mittel, enthaltend eine Kombination aus mindestens einem der unter a) und mindestens einem der unter b) aufgeführten Wirkstoffe: a) Extrakt aus Quassia Amara; b) gesättigte oder ungesättigte, lineare (C9- bis C18)-Dicarbonsäure, insbesondere 8-Hexadecen-1,16-dicarbonsäure und/oder 7-Tetradecen-1,14-dicarbonsäure und/oder 9-Octadecen-1,18-dicarbonsäure und/oder 6-Dodecen-1,12-dicarbonsäure und/oder 5-Decen-1,10-dicarbonsäure und/oder Decandisäure (Sebacinsäure) und/oder Nonandisäure (Azelainsäure), ganz besonders bevorzugt 8-Hexadecen-1,16-dicarbonsäure. Cosmetic or dermatological agent containing a combination of at least one of the active substances listed under a) and at least one of the substances listed under b): a) Extract from Quassia Amara; b) saturated or unsaturated, linear (C9 to C18) dicarboxylic acid, in particular 8-hexadecene-1,16-dicarboxylic acid and / or 7-tetradecene-1,14-dicarboxylic acid and / or 9-octadecene-1,18-dicarboxylic acid and / or 6-dodecene-1,12-dicarboxylic acid and / or 5-decene-1,10-dicarboxylic acid and / or decanedioic acid (sebacic acid) and / or nonanedioic acid (azelaic acid), very particularly preferably 8-hexadecene-1,16- dicarboxylic acid. Mittel nach Anspruch 1, dadurch gekennzeichnet, dass es, bezogen auf sein Gesamtgewicht, insgesamt 0,001 bis 2,0 Gew.-%, vorzugsweise 0,01 bis 0,5 Gew.-% und insbesondere 0,05 bis 0,2 Gew.-% mindestens eines Extraktes aus Quassia Amara enthält.Composition according to claim 1, characterized in that , based on its total weight, a total of 0.001 to 2.0 wt .-%, preferably 0.01 to 0.5 wt .-% and in particular 0.05 to 0.2 wt. - contains at least one extract from Quassia Amara. Mittel nach einem der Ansprüche 1 - 2, dadurch gekennzeichnet, dass es, bezogen auf sein Gesamtgewicht, die gesättigte oder ungesättigte, lineare (C9- bis C18)-Dicarbonsäure, insbesondere die 8-Hexadecen-1,16-dicarbonsäure, in einer Gesamtmenge von 0,01 - 10 Gew.-%, vorzugsweise 0,05 bis 1 Gew.-% und insbesondere 0,1 bis 0,5 Gew.-%, enthält.Composition according to one of claims 1 - 2, characterized in that it, based on its total weight, the saturated or unsaturated, linear (C9 to C18) dicarboxylic acid, in particular the 8-hexadecene-1,16-dicarboxylic acid, in a total amount from 0.01 to 10 wt .-%, preferably 0.05 to 1 wt .-% and in particular 0.1 to 0.5 wt .-%, contains. Mittel nach einem der Ansprüche 1 - 3, dadurch gekennzeichnet, dass das Gewichtsverhältnis des Gesamtgehalts an Extrakt aus Quassia Amara zur Gesamtmenge der gesättigten oder ungesättigten, linearen (C9- bis C18)-Dicarbonsäure 1 : 10 bis 5: 1, vorzugsweise 1 : 5 bis 2 : 1 und insbesondere 1 : 3 bis 1 : 1, beträgt.Agent according to one of claims 1-3, characterized in that the weight ratio of the total content of Quassia Amara extract to the total amount of the saturated or unsaturated, linear (C9 to C18) dicarboxylic acid 1:10 to 5: 1, preferably 1: 5 to 2: 1 and in particular 1: 3 to 1: 1, is. Mittel nach einem der Ansprüche 1 - 4, dadurch gekennzeichnet, dass es zusätzlich insgesamt 0,01 bis 5 Gew.-%, vorzugsweise 0,1 bis 1 Gew.-%, an mindestens einer weiteren hautaufhellenden Substanz enthält, die ausgewählt ist aus der Gruppe, bestehend aus Ascorbinsäure, Ascorbinsäuresalzen, Ascorbinsäureglycosiden, Ascorbinsäureglycosidsalzen, Ascorbinsäureestern von organischen Säuren, den Salzen der Ascorbinsäureester von organischen Säuren, Ascorbinsäureestern von anorganischen Säuren, den Salzen der Ascorbinsäureester von anorganischen Säuren, sowie Mischungen der vorgenannten Substanzen, insbesondere Ascorbinsäure.Agent according to one of claims 1 - 4, characterized in that it additionally contains a total of 0.01 to 5 wt .-%, preferably 0.1 to 1 wt .-%, of at least one further skin lightening substance, which is selected from A group consisting of ascorbic acid, ascorbic acid salts, ascorbic acid glycosides, ascorbic acid glycoside salts, ascorbic acid esters of organic acids, the salts of ascorbic acid esters of organic acids, ascorbic acid esters of inorganic acids, the salts of ascorbic acid esters of inorganic acids, and mixtures of the aforementioned substances, in particular ascorbic acid. Mittel nach einem der Ansprüche 1 - 5, dadurch gekennzeichnet, dass es mindestens ein Metalloxid, vorzugsweise ein Metalloxid als hautaufhellenden Wirkstoff, enthält.Agent according to one of claims 1-5, characterized in that it contains at least one metal oxide, preferably a metal oxide as skin-lightening agent. Mittel nach Anspruch 6, dadurch gekennzeichnet, dass es, bezogen auf sein Gesamtgewicht, insgesamt 0,01 bis 5 Gew.-%, vorzugsweise 0,1 bis 3 Gew.-% Metalloxid, bevorzugt Metalloxid als hautaufhellenden Wirkstoff enthält.Composition according to claim 6, characterized in that it contains, based on its total weight, a total of 0.01 to 5 wt .-%, preferably 0.1 to 3 wt .-% metal oxide, preferably metal oxide as a skin lightening agent. Mittel nach einem der Ansprüche 1 - 7, dadurch gekennzeichnet, dass es 10 bis 80 Gew.-%, vorzugsweise 20 bis 75 Gew.-%, weiter bevorzugt 30 bis 70 Gew.-%, noch weiter bevorzugt 35 bis 60 Gew.-% und insbesondere 40 bis 60 Gew.-% Wasser enthält.Agent according to one of claims 1-7, characterized in that it contains 10 to 80 wt .-%, preferably 20 to 75 wt .-%, more preferably 30 to 70 wt .-%, still more preferably 35 to 60 wt. % and in particular 40 to 60 wt .-% water. Nicht-therapeutische, kosmetische Verwendung eines kosmetischen oder dermatologischen Mittels nach einem der Ansprüche 1 - 8 zur Aufhellung der Hautfarbe, zur Reduzierung der Pigmentierung der Haut, zum Ausgleich des Erscheinungsbildes einer ungleichmäßigen Hautpigmentierung und/oder zur Aufhellung von Altersflecken oder Sommersprossen der Haut.Non-therapeutic, cosmetic use of a cosmetic or dermatological composition according to any one of claims 1-8 for lightening the color of the skin, reducing the pigmentation of the skin, balancing the appearance of uneven skin pigmentation and / or lightening age spots or freckles of the skin. Nicht-therapeutisches, kosmetisches Verfahren zur Aufhellung der Hautfarbe, zur Reduzierung der Pigmentierung der Haut, zum Ausgleich des Erscheinungsbildes einer ungleichmäßigen Hautpigmentierung und/oder zur Aufhellung von Altersflecken oder Sommersprossen der Haut, dadurch gekennzeichnet, dass ein kosmetisches Mittel, enthaltend eine Kombination aus mindestens einem der unter a) und mindestens einem der unter b) aufgeführten Wirkstoffe: a) Extrakt aus Quassia Amara; b) gesättigte oder ungesättigte, lineare (C9- bis C18)-Dicarbonsäure, insbesondere 8-Hexadecen-1,16-dicarbonsäure und/oder 7-Tetradecen-1, 14-dicarbonsäure und/oder 9-Octadecen-1,18-dicarbonsäure und/oder 6-Dodecen-1,12-dicarbonsäure und/oder 5-Decen-1,10-dicarbonsäure und/oder Decandisäure (Sebacinsäure) und/oder Nonandisäure (Azelainsäure), ganz besonders bevorzugt 8-Hexadecen-1,16-dicarbonsäure, auf die Haut aufgetragen wird.Non-therapeutic, cosmetic method for lightening the color of the skin, for reducing the pigmentation of the skin, for balancing the appearance of uneven skin pigmentation and / or for lightening age spots or freckles of the skin, characterized in that a cosmetic agent containing a combination of at least one of the active substances listed under a) and at least one of the substances listed under b): a) Extract from Quassia Amara; b) saturated or unsaturated, linear (C9 to C18) dicarboxylic acid, in particular 8-hexadecene-1,16-dicarboxylic acid and / or 7-tetradecene-1, 14-dicarboxylic acid and / or 9-octadecene-1,18-dicarboxylic acid and / or 6-dodecene-1,12-dicarboxylic acid and / or 5-decene-1,10-dicarboxylic acid and / or decanedioic acid (sebacic acid) and / or nonanedioic acid (azelaic acid), very particularly preferably 8-hexadecene-1,16- dicarboxylic acid, is applied to the skin.
EP14157686.8A 2013-10-09 2014-03-04 Cosmetic or dermatological composition for lightening and for preventing skin blemishes Active EP2862562B1 (en)

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WO2017036650A1 (en) * 2015-08-31 2017-03-09 Henkel Ag & Co. Kgaa Cosmetic o/w emulsions for lightening skin
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US11642290B2 (en) 2017-12-29 2023-05-09 Conopco, Inc. Non-spherical microcapsule
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